1-Cyclopropyl-6-fluoro-8-methoxy-7-(4aS,7aS)-octahydro-pyrrolo[3,4-b]pyridin-6-yl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid

ID: ALA32

Chembl Id: CHEMBL32

Max Phase: Approved

First Approval: 1999

Molecular Formula: C21H24FN3O4

Molecular Weight: 401.44

Molecule Type: Small molecule

Names and Identifiers

Synonyms: Avelox | Avelox iv | Moxifloxacin | Vigamox | Zimoxin

Synonyms from Alternative Forms(13): Moxifloxacin hydrochloride | Moxifloxacin (as hydrochloride) | Moxifloxacin hcl | AL-15469A | BAY 12-8039 | BAY-12-8039 | NSC-758875 | Avelox | Minims | Moxeza | Moxivig | Vigamox | Moxifloxacin Hydrochloride Hydrate

Trade Names(2): Avelox | Avelox i.v.

Canonical SMILES:  COc1c(N2C[C@@H]3CCCN[C@@H]3C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12

Standard InChI:  InChI=1S/C21H24FN3O4/c1-29-20-17-13(19(26)14(21(27)28)9-25(17)12-4-5-12)7-15(22)18(20)24-8-11-3-2-6-23-16(11)10-24/h7,9,11-12,16,23H,2-6,8,10H2,1H3,(H,27,28)/t11-,16+/m0/s1

Standard InChI Key:  FABPRXSRWADJSP-MEDUHNTESA-N

Alternative Forms

1. Parent:

   

   ALA32

   MOXIFLOXACIN

2. Alternative Forms:

   

   ALA32

   Moxifloxacin HCl
3. 

   ALA32

   Moxifloxacin Hydrochloride Monohydrate
4. 

   ALA32

   ---

Molecule Features

Natural Product: Yes

Oral: Yes

Chemical Probe: No

Parenteral: Yes

Molecule Type: Small molecule

Topical: Yes

First In Class: No

Black Box: Yes

Chirality: Yes

Availability: Yes

Prodrug: No

Calculated Properties

Molecular Weight: 401.44

Molecular Weight (Monoisotopic): 401.1751

AlogP: 2.37

#Rotatable Bonds: 4

Polar Surface Area: 83.80

Molecular Species: ZWITTERION

HBA: 6

HBD: 2

#RO5 Violations: 0

HBA (Lipinski): 7

HBD (Lipinski): 2

#RO5 Violations (Lipinski): 0

CX Acidic pKa: 5.49

CX Basic pKa: 9.42

CX LogP: -0.50

CX LogD: -0.50

Aromatic Rings: 2

Heavy Atoms: 29

QED Weighted: 0.82

Np Likeness Score: 0.08

References

1. Inagaki H, Miyauchi S, Miyauchi RN, Kawato HC, Ohki H, Matsuhashi N, Kawakami K, Takahashi H, Takemura M..  (2003)  Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.,  46  (6): [PMID:12620077] [10.1021/jm020328y]

2. Keserü GM..  (2003)  Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.,  13  (16): [PMID:12873512] [10.1016/s0960-894x(03)00492-x]

3. Anquetin G, Rouquayrol M, Mahmoudi N, Santillana-Hayat M, Gozalbes R, Greiner J, Farhati K, Derouin F, Guedj R, Vierling P..  (2004)  Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.,  14  (11): [PMID:15125930] [10.1016/j.bmcl.2004.03.070]

4. Cianchetta G, Mannhold R, Cruciani G, Baroni M, Cecchetti V..  (2004)  Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.,  47  (12): [PMID:15163198] [10.1021/jm030986y]

5. Cavalli A, Poluzzi E, De Ponti F, Recanatini M..  (2002)  Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.,  45  (18): [PMID:12190308] [10.1021/jm0208875]

6. Zloh M, Kaatz GW, Gibbons S..  (2004)  Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.,  14  (4): [PMID:15012986] [10.1016/j.bmcl.2003.12.015]

7. Rajamani R, Tounge BA, Li J, Reynolds CH..  (2005)  A two-state homology model of the hERG K+ channel: application to ligand binding.,  15  (6): [PMID:15745831] [10.1016/j.bmcl.2005.01.008]

8. Inagaki H, Takahashi H, Takemura M..  (2004)  Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.,  14  (20): [PMID:15380226] [10.1016/j.bmcl.2004.07.064]

9. de Souza NJ, Gupte SV, Deshpande PK, Desai VN, Bhawsar SB, Yeole RD, Shukla MC, Strahilevitz J, Hooper DC, Bozdogan B, Appelbaum PC, Jacobs MR, Shetty N, Patel MV, Jha R, Khorakiwala HF..  (2005)  A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.,  48  (16): [PMID:16078842] [10.1021/jm050035f]

10. Tobita M, Nishikawa T, Nagashima R..  (2005)  A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.,  15  (11): [PMID:15911273] [10.1016/j.bmcl.2005.03.080]

11. Wiles JA, Song Y, Wang Q, Lucien E, Hashimoto A, Cheng J, Marlor CW, Ou Y, Podos SD, Thanassi JA, Thoma CL, Deshpande M, Pucci MJ, Bradbury BJ..  (2006)  Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.,  16  (5): [PMID:16337789] [10.1016/j.bmcl.2005.11.064]

12. Wiles JA, Wang Q, Lucien E, Hashimoto A, Song Y, Cheng J, Marlor CW, Ou Y, Podos SD, Thanassi JA, Thoma CL, Deshpande M, Pucci MJ, Bradbury BJ..  (2006)  Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.,  16  (5): [PMID:16337791] [10.1016/j.bmcl.2005.11.065]

13. Wang Q, Lucien E, Hashimoto A, Pais GC, Nelson DM, Song Y, Thanassi JA, Marlor CW, Thoma CL, Cheng J, Podos SD, Ou Y, Deshpande M, Pucci MJ, Buechter DD, Bradbury BJ, Wiles JA..  (2007)  Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.,  50  (2): [PMID:17228862] [10.1021/jm060844e]

14. Nielsen EI, Viberg A, Löwdin E, Cars O, Karlsson MO, Sandström M..  (2007)  Semimechanistic pharmacokinetic/pharmacodynamic model for assessment of activity of antibacterial agents from time-kill curve experiments.,  51  (1): [PMID:17060524] [10.1128/aac.00604-06]

15. Pai H, Seo MR, Choi TY..  (2007)  Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.,  51  (1): [PMID:17074790] [10.1128/aac.00841-06]

16. Duewelhenke N, Krut O, Eysel P..  (2007)  Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.,  51  (1): [PMID:17088489] [10.1128/aac.00729-05]

17. Kosowska-Shick K, Credito KL, Pankuch GA, DeWasse B, McGhee P, Appelbaum PC..  (2007)  Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.,  51  (2): [PMID:17116666] [10.1128/aac.01150-06]

18. Rozen DE, McGee L, Levin BR, Klugman KP..  (2007)  Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.,  51  (2): [PMID:17116668] [10.1128/aac.01161-06]

19. Shandil RK, Jayaram R, Kaur P, Gaonkar S, Suresh BL, Mahesh BN, Jayashree R, Nandi V, Bharath S, Balasubramanian V..  (2007)  Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.,  51  (2): [PMID:17145798] [10.1128/aac.00414-06]

20. Vidaillac C, Guillon J, Arpin C, Forfar-Bares I, Ba BB, Grellet J, Moreau S, Caignard DH, Jarry C, Quentin C..  (2007)  Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.,  51  (3): [PMID:17101679] [10.1128/aac.01306-05]

21. Frank KL, Reichert EJ, Piper KE, Patel R..  (2007)  In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.,  51  (3): [PMID:17158933] [10.1128/aac.01052-06]

22. Ibrahim M, Andries K, Lounis N, Chauffour A, Truffot-Pernot C, Jarlier V, Veziris N..  (2007)  Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.,  51  (3): [PMID:17178794] [10.1128/aac.00898-06]

23. Cercenado E, Marín M, Sánchez-Martínez M, Cuevas O, Martínez-Alarcón J, Bouza E..  (2007)  In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.,  51  (3): [PMID:17194827] [10.1128/aac.01102-06]

24. Cho SH, Warit S, Wan B, Hwang CH, Pauli GF, Franzblau SG..  (2007)  Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.,  51  (4): [PMID:17210775] [10.1128/aac.00055-06]

25. Hong SG, Moland ES, Wickman PA, Black JA, Hossain A, Hanson ND, Thomson KS..  (2007)  In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.,  51  (4): [PMID:17220419] [10.1128/aac.00959-06]

26. Pucci MJ, Cheng J, Podos SD, Thoma CL, Thanassi JA, Buechter DD, Mushtaq G, Vigliotti GA, Bradbury BJ, Deshpande M..  (2007)  In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.,  51  (4): [PMID:17242152] [10.1128/aac.01315-06]

27. Pérez-Vázquez M, Román F, García-Cobos S, Campos J..  (2007)  Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.,  51  (4): [PMID:17283196] [10.1128/aac.01437-06]

28. LaPlante KL, Rybak MJ, Tsuji B, Lodise TP, Kaatz GW..  (2007)  Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.,  51  (4): [PMID:17296740] [10.1128/aac.00646-06]

29. Moda TL, Montanari CA, Andricopulo AD..  (2007)  Hologram QSAR model for the prediction of human oral bioavailability.,  15  (24): [PMID:17870541] [10.1016/j.bmc.2007.08.060]

30. Stucki A, Cottagnoud M, Winkelmann V, Schaffner T, Cottagnoud P..  (2007)  Daptomycin produces an enhanced bactericidal activity compared to ceftriaxone, measured by [3H]choline release in the cerebrospinal fluid, in experimental meningitis due to a penicillin-resistant pneumococcal strain without lysing its cell wall.,  51  (6): [PMID:17371817] [10.1128/aac.01000-06]

31. Snydman DR, Jacobus NV, McDermott LA, Ruthazer R, Golan Y, Goldstein EJ, Finegold SM, Harrell LJ, Hecht DW, Jenkins SG, Pierson C, Venezia R, Yu V, Rihs J, Gorbach SL..  (2007)  National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.,  51  (5): [PMID:17283189] [10.1128/aac.01435-06]

32. Könönen E, Bryk A, Niemi P, Kanervo-Nordström A..  (2007)  Antimicrobial susceptibilities of Peptostreptococcus anaerobius and the newly described Peptostreptococcus stomatis isolated from various human sources.,  51  (6): [PMID:17403999] [10.1128/aac.00056-07]

33. Rodríguez-Martínez JM, Velasco C, García I, Cano ME, Martínez-Martínez L, Pascual A..  (2007)  Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.,  51  (6): [PMID:17404007] [10.1128/aac.01444-06]

34. Matrat S, Petrella S, Cambau E, Sougakoff W, Jarlier V, Aubry A..  (2007)  Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.,  51  (5): [PMID:17325221] [10.1128/aac.01282-06]

35. Weiner M, Burman W, Luo CC, Peloquin CA, Engle M, Goldberg S, Agarwal V, Vernon A..  (2007)  Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.,  51  (8): [PMID:17517835] [10.1128/aac.01621-06]

36. Hecht DW, Galang MA, Sambol SP, Osmolski JR, Johnson S, Gerding DN..  (2007)  In vitro activities of 15 antimicrobial agents against 110 toxigenic clostridium difficile clinical isolates collected from 1983 to 2004.,  51  (8): [PMID:17517836] [10.1128/aac.01623-06]

37. Skiadas I, Pefanis A, Papalois A, Kyroudi A, Triantafyllidi H, Tsaganos T, Giamarellou H..  (2007)  Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.,  51  (8): [PMID:17562794] [10.1128/aac.01376-06]

38. Adams DA, Riggs MM, Donskey CJ..  (2007)  Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.,  51  (8): [PMID:17562807] [10.1128/aac.01582-06]

39. Jia L, Sun H..  (2008)  Support vector machines classification of hERG liabilities based on atom types.,  16  (11): [PMID:18448342] [10.1016/j.bmc.2008.04.028]

40. Yamane K, Wachino J, Suzuki S, Kimura K, Shibata N, Kato H, Shibayama K, Konda T, Arakawa Y..  (2007)  New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.,  51  (9): [PMID:17548499] [10.1128/aac.00339-07]

41. Arsène S, Leclercq R..  (2007)  Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.,  51  (9): [PMID:17620379] [10.1128/aac.00274-07]

42. Calatayud L, Ardanuy C, Cercenado E, Fenoll A, Bouza E, Pallares R, Martín R, Liñares J..  (2007)  Serotypes, Clones, and Mechanisms of Resistance of Erythromycin-Resistant Streptococcus pneumoniae Isolates Collected in Spain.,  51  (9): [PMID:17606677] [10.1128/aac.00157-07]

43. Grossi O, Caillon J, Arvieux C, Jacqueline C, Bugnon D, Potel G, Hamel A..  (2007)  In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.,  51  (9): [PMID:17576849] [10.1128/aac.01520-06]

44. Ji B, Chauffour A, Robert J, Lefrançois S, Jarlier V..  (2007)  Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.,  51  (10): [PMID:17664316] [10.1128/aac.00730-07]

45. Kohno Y, Ohno H, Miyazaki Y, Higashiyama Y, Yanagihara K, Hirakata Y, Fukushima K, Kohno S..  (2007)  In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.,  51  (11): [PMID:17709469] [10.1128/aac.00410-07]

46. Shin JH, Jung HJ, Kim HR, Jeong J, Jeong SH, Kim S, Lee EY, Lee JN, Chang CL..  (2007)  Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.,  51  (7): [PMID:17502407] [10.1128/aac.00107-07]

47. Cattoir V, Poirel L, Nordmann P..  (2007)  Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.,  51  (7): [PMID:17502413] [10.1128/aac.01616-06]

48. Périchon B, Courvalin P, Galimand M..  (2007)  Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.,  51  (7): [PMID:17470656] [10.1128/aac.00143-07]

49. Cheng J, Thanassi JA, Thoma CL, Bradbury BJ, Deshpande M, Pucci MJ..  (2007)  Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.,  51  (7): [PMID:17502409] [10.1128/aac.00158-07]

50. Cattoir V, Poirel L, Mazel D, Soussy CJ, Nordmann P..  (2007)  Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.,  51  (7): [PMID:17452482] [10.1128/aac.00070-07]

51. Tanaka KS, Houghton TJ, Kang T, Dietrich E, Delorme D, Ferreira SS, Caron L, Viens F, Arhin FF, Sarmiento I, Lehoux D, Fadhil I, Laquerre K, Liu J, Ostiguy V, Poirier H, Moeck G, Parr TR, Rafai Far A..  (2008)  Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.,  16  (20): [PMID:18815051] [10.1016/j.bmc.2008.09.010]

52. Houghton TJ, Tanaka KS, Kang T, Dietrich E, Lafontaine Y, Delorme D, Ferreira SS, Viens F, Arhin FF, Sarmiento I, Lehoux D, Fadhil I, Laquerre K, Liu J, Ostiguy V, Poirier H, Moeck G, Parr TR, Far AR..  (2008)  Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.,  51  (21): [PMID:18834106] [10.1021/jm801007z]

53. Ermondi G, Visentin S, Caron G..  (2009)  GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.,  44  (5): [PMID:19110341] [10.1016/j.ejmech.2008.11.009]

54. Mo S, Krunic A, Chlipala G, Orjala J..  (2009)  Antimicrobial ambiguine isonitriles from the cyanobacterium Fischerella ambigua.,  72  (5): [PMID:19371071] [10.1021/np800751j]

55. Clark CL, Kosowska-Shick K, Ednie LM, Appelbaum PC..  (2007)  Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.,  51  (11): [PMID:17876003] [10.1128/aac.00827-07]

56. Morio F, Jean-Pierre H, Dubreuil L, Jumas-Bilak E, Calvet L, Mercier G, Devine R, Marchandin H..  (2007)  Antimicrobial susceptibilities and clinical sources of Dialister species.,  51  (12): [PMID:17923492] [10.1128/aac.00538-07]

57. Quiroga MP, Andres P, Petroni A, Soler Bistué AJ, Guerriero L, Vargas LJ, Zorreguieta A, Tokumoto M, Quiroga C, Tolmasky ME, Galas M, Centrón D..  (2007)  Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.,  51  (12): [PMID:17938184] [10.1128/aac.00726-07]

58. Clark C, Smith K, Ednie L, Bogdanovich T, Dewasse B, McGhee P, Appelbaum PC..  (2008)  In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.,  52  (1): [PMID:17938189] [10.1128/aac.01229-07]

59. Almeida D, Nuermberger E, Tyagi S, Bishai WR, Grosset J..  (2007)  In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.,  51  (12): [PMID:17938193] [10.1128/aac.01123-07]

60. Varma MV, Feng B, Obach RS, Troutman MD, Chupka J, Miller HR, El-Kattan A..  (2009)  Physicochemical determinants of human renal clearance.,  52  (15): [PMID:19445515] [10.1021/jm900403j]

61. Damier-Piolle L, Magnet S, Brémont S, Lambert T, Courvalin P..  (2008)  AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.,  52  (2): [PMID:18086852] [10.1128/aac.00732-07]

62. Homma T, Hori T, Sugimori G, Yamano Y..  (2007)  Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.,  51  (11): [PMID:17664314] [10.1128/aac.01372-06]

63. Morgan-Linnell SK, Zechiedrich L..  (2007)  Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.,  51  (11): [PMID:17682104] [10.1128/aac.00647-07]

64. Matrat S, Cambau E, Jarlier V, Aubry A..  (2008)  Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?,  52  (2): [PMID:18070975] [10.1128/aac.01095-07]

65. Azéma J, Guidetti B, Dewelle J, Le Calve B, Mijatovic T, Korolyov A, Vaysse J, Malet-Martino M, Martino R, Kiss R..  (2009)  7-((4-Substituted)piperazin-1-yl) derivatives of ciprofloxacin: synthesis and in vitro biological evaluation as potential antitumor agents.,  17  (15): [PMID:19595598] [10.1016/j.bmc.2009.06.053]

66. Dubar F, Anquetin G, Pradines B, Dive D, Khalife J, Biot C..  (2009)  Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.,  52  (24): [PMID:19908867] [10.1021/jm901357n]

67. Pieroni M, Lilienkampf A, Wan B, Wang Y, Franzblau SG, Kozikowski AP..  (2009)  Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.,  52  (20): [PMID:19757815] [10.1021/jm900513a]

68. Varma MV, Obach RS, Rotter C, Miller HR, Chang G, Steyn SJ, El-Kattan A, Troutman MD..  (2010)  Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.,  53  (3): [PMID:20070106] [10.1021/jm901371v]

69. Miyauchi R, Kawakami K, Ito M, Matsuhashi N, Ohki H, Inagaki H, Takahashi H, Takemura M..  (2009)  Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.,  17  (19): [PMID:19736016] [10.1016/j.bmc.2009.08.026]

70. Hans RH, Guantai EM, Lategan C, Smith PJ, Wan B, Franzblau SG, Gut J, Rosenthal PJ, Chibale K..  (2010)  Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.,  20  (3): [PMID:20045640] [10.1016/j.bmcl.2009.12.062]

71. Pieroni M, Dimovska M, Brincat JP, Sabatini S, Carosati E, Massari S, Kaatz GW, Fravolini A..  (2010)  From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.,  53  (11): [PMID:20446747] [10.1021/jm1003304]

72. Schneemann I, Kajahn I, Ohlendorf B, Zinecker H, Erhard A, Nagel K, Wiese J, Imhoff JF..  (2010)  Mayamycin, a cytotoxic polyketide from a Streptomyces strain isolated from the marine sponge Halichondria panicea.,  73  (7): [PMID:20545334] [10.1021/np100135b]

73. Feng LS, Liu ML, Wang B, Chai Y, Hao XQ, Meng S, Guo HY..  (2010)  Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.,  45  (8): [PMID:20493593] [10.1016/j.ejmech.2010.04.027]

74. Brillault J, De Castro WV, Couet W..  (2010)  Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.,  54  (1): [PMID:19822706] [10.1128/aac.00733-09]

75. Sánchez MB, Martínez JL..  (2010)  SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.,  54  (1): [PMID:19841154] [10.1128/aac.00496-09]

76. Montes M, Tamayo E, Orden B, Larruskain J, Perez-Trallero E..  (2010)  Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.,  54  (1): [PMID:19805559] [10.1128/aac.00780-09]

77. Credito K, Kosowska-Shick K, McGhee P, Pankuch GA, Appelbaum PC..  (2010)  Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.,  54  (2): [PMID:20008781] [10.1128/aac.01353-09]

78. Al-Trawneh SA, Zahra JA, Kamal MR, El-Abadelah MM, Zani F, Incerti M, Cavazzoni A, Alfieri RR, Petronini PG, Vicini P..  (2010)  Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.,  18  (16): [PMID:20667744] [10.1016/j.bmc.2010.06.098]

79. McGhee P, Clark C, Kosowska-Shick KM, Nagai K, Dewasse B, Beachel L, Appelbaum PC..  (2010)  In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.,  54  (1): [PMID:19884376] [10.1128/aac.01123-09]

80. Lauderdale TL, Shiau YR, Lai JF, Chen HC, King CH..  (2010)  Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.,  54  (3): [PMID:20065058] [10.1128/aac.01197-09]

81. Khoje AD, Kulendrn A, Charnock C, Wan B, Franzblau S, Gundersen LL..  (2010)  Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.,  18  (20): [PMID:20833056] [10.1016/j.bmc.2010.08.016]

82. Morrow BJ, He W, Amsler KM, Foleno BD, Macielag MJ, Lynch AS, Bush K..  (2010)  In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.,  54  (5): [PMID:20176911] [10.1128/aac.01374-09]

83. Disratthakit A, Doi N..  (2010)  In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.,  54  (6): [PMID:20368403] [10.1128/aac.01545-09]

84. Lenaerts AJ, Bitting C, Woolhiser L, Gruppo V, Marietta KS, Johnson CM, Orme IM..  (2008)  Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.,  52  (4): [PMID:18268091] [10.1128/aac.00897-07]

85. Daw-Garza A, Welsh O, Said-Fernández S, Lozano-Garza HG, Waksman de Torres N, Rocha NC, Ocampo-Candiani J, Vera-Cabrera L..  (2008)  In vivo therapeutic effect of gatifloxacin on BALB/c mice infected with Nocardia brasiliensis.,  52  (4): [PMID:18285484] [10.1128/aac.00148-08]

86. Wu HM, Janapatla RP, Ho YR, Hung KH, Wu CW, Yan JJ, Wu JJ..  (2008)  Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.,  52  (5): [PMID:18299411] [10.1128/aac.00035-08]

87. Lehtopolku M, Nakari UM, Kotilainen P, Huovinen P, Siitonen A, Hakanen AJ..  (2010)  Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.,  54  (3): [PMID:20038624] [10.1128/aac.00898-09]

88. Grayo S, Join-Lambert O, Desroches MC, Le Monnier A..  (2008)  Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.,  52  (5): [PMID:18299415] [10.1128/aac.01211-07]

89. Hsieh YC, Chang KY, Huang YC, Lin HC, Ho YH, Huang LM, Hsueh PR..  (2008)  Clonal spread of highly beta-lactam-resistant Streptococcus pneumoniae isolates in Taiwan.,  52  (6): [PMID:18413298] [10.1128/aac.00046-08]

90. Rullas J, García JI, Beltrán M, Cardona PJ, Cáceres N, García-Bustos JF, Angulo-Barturen I..  (2010)  Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.,  54  (5): [PMID:20160054] [10.1128/aac.01423-09]

91. Alffenaar JW, de Vries PM, Luijckx GJ, van Soolingen D, van der Werf TS, van Altena R..  (2008)  Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.,  52  (6): [PMID:18362186] [10.1128/aac.01637-07]

92. Deshpande D, Srivastava S, Meek C, Leff R, Hall GS, Gumbo T..  (2010)  Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.,  54  (6): [PMID:20385862] [10.1128/aac.01761-09]

93. O'Mara E, Kasserra C, Huddlestone JR, Wan Y, Soni P, Caceres M, Medlock M, Morrison R, Devinsky O..  (2010)  Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.,  54  (6): [PMID:20350942] [10.1128/aac.01447-09]

94. Zhanel GG, DeCorby M, Laing N, Weshnoweski B, Vashisht R, Tailor F, Nichol KA, Wierzbowski A, Baudry PJ, Karlowsky JA, Lagacé-Wiens P, Walkty A, McCracken M, Mulvey MR, Johnson J, Canadian Antimicrobial Resistance Alliance (CARA), Hoban DJ..  (2008)  Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.,  52  (4): [PMID:18285482] [10.1128/aac.01538-07]

95. Peloquin CA, Hadad DJ, Molino LP, Palaci M, Boom WH, Dietze R, Johnson JL..  (2008)  Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.,  52  (3): [PMID:18070980] [10.1128/aac.01036-07]

96. Ressner RA, Griffith ME, Beckius ML, Pimentel G, Miller RS, Mende K, Fraser SL, Galloway RL, Hospenthal DR, Murray CK..  (2008)  Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.,  52  (8): [PMID:18411316] [10.1128/aac.00044-08]

97. Matrat S, Aubry A, Mayer C, Jarlier V, Cambau E..  (2008)  Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.,  52  (8): [PMID:18426901] [10.1128/aac.01380-07]

98. Betriu C, Culebras E, Gómez M, López F, Rodríguez-Avial I, Picazo JJ..  (2008)  Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.,  52  (7): [PMID:18474575] [10.1128/aac.00081-08]

99. Karlowsky JA, Laing NM, Zhanel GG..  (2008)  In vitro activity of OPT-80 tested against clinical isolates of toxin-producing Clostridium difficile.,  52  (11): [PMID:18725442] [10.1128/aac.00476-08]

100. Cattoir V, Poirel L, Nordmann P..  (2008)  Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.,  52  (10): [PMID:18644958] [10.1128/aac.00638-08]

101. Shimizu K, Kikuchi K, Sasaki T, Takahashi N, Ohtsuka M, Ono Y, Hiramatsu K..  (2008)  Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.,  52  (10): [PMID:18644963] [10.1128/aac.00026-08]

102. German N, Malik M, Rosen JD, Drlica K, Kerns RJ..  (2008)  Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones.,  52  (11): [PMID:18765690] [10.1128/aac.00330-08]

103. Zhang T, Bishai WR, Grosset JH, Nuermberger EL..  (2010)  Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.,  54  (7): [PMID:20421401] [10.1128/aac.00400-10]

104. Snydman DR, Jacobus NV, McDermott LA..  (2008)  In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.,  52  (12): [PMID:18838581] [10.1128/aac.00696-08]

105. Pucci MJ, Ackerman M, Thanassi JA, Shoen CM, Cynamon MH..  (2010)  In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.,  54  (8): [PMID:20516287] [10.1128/aac.00287-10]

106. Waites KB, Crabb DM, Duffy LB..  (2008)  Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.,  52  (10): [PMID:18663020] [10.1128/aac.00849-08]

107. Zapor MJ, Barber M, Summers A, Miller GH, Feeney LA, Eberly LE, Wortmann G..  (2010)  In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.,  54  (7): [PMID:20404121] [10.1128/aac.01173-09]

108. Pires R, Ardanuy C, Rolo D, Morais A, Brito-Avô A, Gonçalo-Marques J, Liñares J, Santos-Sanches I..  (2010)  Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.,  54  (6): [PMID:20350943] [10.1128/aac.01536-09]

109. Ward KW, Nagilla R, Jolivette LJ..  (2005)  Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.,  35  (2): [PMID:16019946] [10.1080/00498250400028197]

110. Obach RS, Lombardo F, Waters NJ..  (2008)  Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.,  36  (7): [PMID:18426954] [10.1124/dmd.108.020479]

111. Jolivette LJ, Ward KW..  (2005)  Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.,  94  (7): [PMID:15920768] [10.1002/jps.20373]

112. del Pozo JL, Rouse MS, Mandrekar JN, Sampedro MF, Steckelberg JM, Patel R..  (2009)  Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.,  53  (1): [PMID:18725436] [10.1128/aac.00237-08]

113. Page S, Vernel-Pauillac F, O'Connor O, Bremont S, Charavay F, Courvalin P, Goarant C, Le Hello S..  (2008)  Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.,  52  (11): [PMID:18725440] [10.1128/aac.00082-08]

114. Chacon-Moreno BE, Welsh O, Cavazos-Rocha N, de la Luz Salazar-Cavazos M, Garza-Lozano HG, Said-Fernandez S, Ocampo-Candiani J, Vera-Cabrera L..  (2009)  Efficacy of ciprofloxacin and moxifloxacin against Nocardia brasiliensis in vitro and in an experimental model of actinomycetoma in BALB/c mice.,  53  (1): [PMID:18852277] [10.1128/aac.01023-08]

115. Grayo S, Lott-Desroches MC, Dussurget O, Respaud R, Fontanet A, Join-Lambert O, Singlas E, Le Monnier A..  (2008)  Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.,  52  (9): [PMID:18573932] [10.1128/aac.00177-08]

116. Bhagwat SS, McGhee P, Kosowska-Shick K, Patel MV, Appelbaum PC..  (2009)  In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.,  53  (2): [PMID:19029326] [10.1128/aac.01150-08]

117. Dionisi AM, Lucarelli C, Owczarek S, Luzzi I, Villa L..  (2009)  Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.,  53  (9): [PMID:19528272] [10.1128/aac.00294-09]

118. Von Groll A, Martin A, Jureen P, Hoffner S, Vandamme P, Portaels F, Palomino JC, da Silva PA..  (2009)  Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.,  53  (10): [PMID:19687244] [10.1128/aac.00287-09]

119. Rao SS, Raghunathan R, Ekambaram R, Raghunathan M..  (2009)  In vitro activity of a new quinoline derivative, ER-2, against clinical isolates of Mycoplasma pneumoniae and Mycoplasma hominis.,  53  (12): [PMID:19738013] [10.1128/aac.00746-09]

120. Hamasuna R, Jensen JS, Osada Y..  (2009)  Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.,  53  (11): [PMID:19738019] [10.1128/aac.00724-09]

121. Bowker KE, Caspers P, Gaucher B, MacGowan AP..  (2009)  In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.,  53  (11): [PMID:19738027] [10.1128/aac.00845-09]

122. MacGowan AP, Reynolds R, Noel AR, Bowker KE..  (2009)  Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.,  53  (12): [PMID:19805569] [10.1128/aac.00118-09]

123. Denève C, Bouttier S, Dupuy B, Barbut F, Collignon A, Janoir C..  (2009)  Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.,  53  (12): [PMID:19805572] [10.1128/aac.00532-09]

124. Saxton K, Baines SD, Freeman J, O'Connor R, Wilcox MH..  (2009)  Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.,  53  (2): [PMID:18710908] [10.1128/aac.00306-08]

125. Brillault J, De Castro WV, Harnois T, Kitzis A, Olivier JC, Couet W..  (2009)  P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.,  53  (4): [PMID:19188390] [10.1128/aac.01253-08]

126. Landersdorfer CB, Kinzig M, Hennig FF, Bulitta JB, Holzgrabe U, Drusano GL, Sörgel F, Gusinde J..  (2009)  Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.,  53  (5): [PMID:19223648] [10.1128/aac.01056-08]

127. Liu Y, Ye X, Zhang H, Xu X, Li W, Zhu D, Wang M..  (2009)  Antimicrobial susceptibility of Mycoplasma pneumoniae isolates and molecular analysis of macrolide-resistant strains from Shanghai, China.,  53  (5): [PMID:19273684] [10.1128/aac.01684-08]

128. Kim ES, Jeong JY, Jun JB, Choi SH, Lee SO, Kim MN, Woo JH, Kim YS..  (2009)  Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.,  53  (6): [PMID:19289526] [10.1128/aac.01534-08]

129. Kosowska-Shick K, Ednie LM, McGhee P, Appelbaum PC..  (2009)  Comparative antipneumococcal activities of sulopenem and other drugs.,  53  (6): [PMID:19307366] [10.1128/aac.01531-08]

130. Spigaglia P, Barbanti F, Louie T, Barbut F, Mastrantonio P..  (2009)  Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.,  53  (6): [PMID:19364867] [10.1128/aac.01252-08]

131. Yamamoto K, Yanagihara K, Sugahara K, Imamura Y, Seki M, Izumikawa K, Kakeya H, Yamamoto Y, Hirakata Y, Kamihira S, Kohno S..  (2009)  In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.,  53  (8): [PMID:19451290] [10.1128/aac.00176-09]

132. Haas W, Pillar CM, Zurenko GE, Lee JC, Brunner LS, Morris TW..  (2009)  Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.,  53  (8): [PMID:19506065] [10.1128/aac.00418-09]

133. Liu CY, Huang YT, Liao CH, Yen LC, Lin HY, Hsueh PR..  (2008)  Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.,  52  (9): [PMID:18625771] [10.1128/aac.00355-08]

134. Dooley K, Flexner C, Hackman J, Peloquin CA, Nuermberger E, Chaisson RE, Dorman SE..  (2008)  Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.,  52  (11): [PMID:18765687] [10.1128/aac.00554-08]

135. Wehmeier C, Schuster S, Fähnrich E, Kern WV, Bohnert JA..  (2009)  Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.,  53  (1): [PMID:18936189] [10.1128/aac.00921-08]

136. Osborne CS, Neckermann G, Fischer E, Pecanka R, Yu D, Manni K, Goldovitz J, Amaral K, Dzink-Fox J, Ryder NS..  (2009)  In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.,  53  (9): [PMID:19596876] [10.1128/aac.00026-09]

137. Gunell M, Webber MA, Kotilainen P, Lilly AJ, Caddick JM, Jalava J, Huovinen P, Siitonen A, Hakanen AJ, Piddock LJ..  (2009)  Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.,  53  (9): [PMID:19596880] [10.1128/aac.00121-09]

138. Adam HJ, Laing NM, King CR, Lulashnyk B, Hoban DJ, Zhanel GG..  (2009)  In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.,  53  (11): [PMID:19738018] [10.1128/aac.00078-09]

139. Xu X, Cai L, Xiao M, Kong F, Oftadeh S, Zhou F, Gilbert GL..  (2010)  Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.,  54  (3): [PMID:20065057] [10.1128/aac.01268-09]

140. Jacobs MR, Good CE, Windau AR, Bajaksouzian S, Biek D, Critchley IA, Sader HS, Jones RN..  (2010)  Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.,  54  (6): [PMID:20308374] [10.1128/aac.01797-09]

141. Lee Y, Park Y, Kim MS, Yong D, Jeong SH, Lee K, Chong Y..  (2010)  Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.,  54  (9): [PMID:20585132] [10.1128/aac.00481-10]

142. Parra-Ruiz J, Vidaillac C, Rose WE, Rybak MJ..  (2010)  Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.,  54  (10): [PMID:20696880] [10.1128/aac.00455-10]

143. Khanna A, Raj VS, Tarai B, Sood R, Pareek PK, Upadhyay DJ, Sharma P, Rattan A, Saini KS, Singh H..  (2010)  Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.,  54  (11): [PMID:20713679] [10.1128/aac.00661-10]

144. Jeong JW, Jung SJ, Lee HH, Kim YZ, Park TK, Cho YL, Chae SE, Baek SY, Woo SH, Lee HS, Kwak JH..  (2010)  In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.,  54  (12): [PMID:20855730] [10.1128/aac.00723-10]

145. Sinha N, Sen S..  (2011)  Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.,  46  (2): [PMID:21185626] [10.1016/j.ejmech.2010.11.042]

146. van den Boogaard J, Kibiki GS, Kisanga ER, Boeree MJ, Aarnoutse RE..  (2009)  New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.,  53  (3): [PMID:19075046] [10.1128/aac.00749-08]

147. Nguyen HA, Denis O, Vergison A, Theunis A, Tulkens PM, Struelens MJ, Van Bambeke F..  (2009)  Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype and revertant strains.,  53  (4): [PMID:19188393] [10.1128/aac.01145-08]

148. Drusano GL, Okusanya OO, Okusanya AO, van Scoy B, Brown DL, Fregeau C, Kulawy R, Kinzig M, Sörgel F, Heine HS, Louie A..  (2009)  Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.,  53  (11): [PMID:19687233] [10.1128/aac.00802-09]

149. Marchand S, Gobin P, Brillault J, Baptista S, Adier C, Olivier JC, Mimoz O, Couet W..  (2010)  Aerosol therapy with colistin methanesulfonate: a biopharmaceutical issue illustrated in rats.,  54  (9): [PMID:20547787] [10.1128/aac.00411-10]

150. Malik M, Marks KR, Schwanz HA, German N, Drlica K, Kerns RJ..  (2010)  Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.,  54  (12): [PMID:20855738] [10.1128/aac.01054-10]

151. Higgins PG, Schneiders T, Hamprecht A, Seifert H..  (2010)  In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.,  54  (12): [PMID:20921306] [10.1128/aac.00598-10]

152. Briales A, Rodríguez-Martínez JM, Velasco C, Díaz de Alba P, Domínguez-Herrera J, Pachón J, Pascual A..  (2011)  In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.,  55  (3): [PMID:21173174] [10.1128/aac.00927-10]

153. Fourches D, Barnes JC, Day NC, Bradley P, Reed JZ, Tropsha A..  (2010)  Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.,  23  (1): [PMID:20014752] [10.1021/tx900326k]

154. Hans RH, Wiid IJ, van Helden PD, Wan B, Franzblau SG, Gut J, Rosenthal PJ, Chibale K..  (2011)  Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents.,  21  (7): [PMID:21376591] [10.1016/j.bmcl.2011.02.008]

155. Al-Trawneh SA, El-Abadelah MM, Zahra JA, Al-Taweel SA, Zani F, Incerti M, Cavazzoni A, Vicini P..  (2011)  Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.,  19  (8): [PMID:21458275] [10.1016/j.bmc.2011.03.018]

156. Kim HY, Wiles JA, Wang Q, Pais GC, Lucien E, Hashimoto A, Nelson DM, Thanassi JA, Podos SD, Deshpande M, Pucci MJ, Bradbury BJ..  (2011)  Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).,  54  (9): [PMID:21425851] [10.1021/jm101604v]

157. Singh K, Singh K, Wan B, Franzblau S, Chibale K, Balzarini J..  (2011)  Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.,  46  (6): [PMID:21450375] [10.1016/j.ejmech.2011.03.010]

158. Wang JX, Zhang YB, Liu ML, Wang B, Chai Y, Li SJ, Guo HY..  (2011)  Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.,  46  (6): [PMID:21481984] [10.1016/j.ejmech.2011.03.026]

159. Macabeo AP, Vidar WS, Chen X, Decker M, Heilmann J, Wan B, Franzblau SG, Galvez EV, Aguinaldo MA, Cordell GA..  (2011)  Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.,  46  (7): [PMID:21546135] [10.1016/j.ejmech.2011.04.025]

160. Marks KR, Malik M, Mustaev A, Hiasa H, Drlica K, Kerns RJ..  (2011)  Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones.,  21  (15): [PMID:21705218] [10.1016/j.bmcl.2011.05.112]

161. Liu Z, Shi Q, Ding D, Kelly R, Fang H, Tong W..  (2011)  Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).,  7  (12): [PMID:22194678] [10.1371/journal.pcbi.1002310]

162. Jin Y, Gill SK, Kirchhoff PD, Wan B, Franzblau SG, Garcia GA, Showalter HD..  (2011)  Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.,  21  (20): [PMID:21903392] [10.1016/j.bmcl.2011.08.054]

163. Lv K, Liu ML, Feng LS, Sun LY, Sun YX, Wei ZQ, Guo HQ..  (2012)  Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.,  47  [PMID:22079379] [10.1016/j.ejmech.2011.10.048]

164. Lu X, Liu X, Wan B, Franzblau SG, Chen L, Zhou C, You Q..  (2012)  Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2.,  49  [PMID:22264895] [10.1016/j.ejmech.2012.01.007]

165. Gill SK, Xu H, Kirchhoff PD, Cierpicki T, Turbiak AJ, Wan B, Zhang N, Peng KW, Franzblau SG, Garcia GA, Showalter HD..  (2012)  Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.,  55  (8): [PMID:22452568] [10.1021/jm201716n]

166. Dulla B, Wan B, Franzblau SG, Kapavarapu R, Reiser O, Iqbal J, Pal M..  (2012)  Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.,  22  (14): [PMID:22726932] [10.1016/j.bmcl.2012.05.096]

167. Pathak RB, Chovatia PT, Parekh HH..  (2012)  Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives.,  22  (15): [PMID:22695129] [10.1016/j.bmcl.2012.05.063]

168. Feng L, Lv K, Liu M, Wang S, Zhao J, You X, Li S, Cao J, Guo H..  (2012)  Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety.,  55  [PMID:22841282] [10.1016/j.ejmech.2012.07.010]

169. USP Dictionary of USAN and International Names (2010 edition) and USAN registrations 2007-date, 

170. Wiles JA, Phadke AS, Bradbury BJ, Pucci MJ, Thanassi JA, Deshpande M..  (2011)  Selenophene-containing inhibitors of type IIA bacterial topoisomerases.,  54  (9): [PMID:21443219] [10.1021/jm2002124]

171. Villemagne B, Crauste C, Flipo M, Baulard AR, Déprez B, Willand N..  (2012)  Tuberculosis: the drug development pipeline at a glance.,  51  [PMID:22421275] [10.1016/j.ejmech.2012.02.033]

172. Murali K, Avinash R, Kirthiga R, Franzblau SG.  (2012)  Synthesis, antibacterial, and antitubercular studies of some novel isatin derivatives,  21  (12): [10.1007/s00044-012-9971-7]

173. Asif M, Siddiqui AA, Husain A.  (2013)  Quinolone derivatives as antitubercular drugs,  22  (3): [10.1007/s00044-012-0101-3]

174. Odagiri T, Inagaki H, Sugimoto Y, Nagamochi M, Miyauchi RN, Kuroyanagi J, Kitamura T, Komoriya S, Takahashi H..  (2013)  Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.,  56  (5): [PMID:23409972] [10.1021/jm301650g]

175. Gomez C, Ponien P, Serradji N, Lamouri A, Pantel A, Capton E, Jarlier V, Anquetin G, Aubry A..  (2013)  Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.,  21  (4): [PMID:23294829] [10.1016/j.bmc.2012.12.011]

176. Ryu S, Imai YN, Oiki S..  (2013)  The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.,  23  (13): [PMID:23711922] [10.1016/j.bmcl.2013.04.074]

177. Guo M, Zheng CJ, Song MX, Wu Y, Sun LP, Li YJ, Liu Y, Piao HR..  (2013)  Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.,  23  (15): [PMID:23787100] [10.1016/j.bmcl.2013.05.082]

178. Dartois V, Barry CE..  (2013)  A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.,  23  (17): [PMID:23910985] [10.1016/j.bmcl.2013.07.006]

179. Settimo L, Bellman K, Knegtel RM..  (2013)  Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.,  [PMID:24249037] [10.1007/s11095-013-1232-z]

180. Shirude PS, Madhavapeddi P, Naik M, Murugan K, Shinde V, Nandishaiah R, Bhat J, Kumar A, Hameed S, Holdgate G, Davies G, McMiken H, Hegde N, Ambady A, Venkatraman J, Panda M, Bandodkar B, Sambandamurthy VK, Read JA..  (2013)  Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.,  56  (21): [PMID:24107081] [10.1021/jm4012033]

181. Liu JC, Zheng CJ, Wang MX, Li YR, Ma LX, Hou SP, Piao HR..  (2014)  Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.,  74  [PMID:24487189] [10.1016/j.ejmech.2013.12.054]

182. Encinas L, O'Keefe H, Neu M, Remuiñán MJ, Patel AM, Guardia A, Davie CP, Pérez-Macías N, Yang H, Convery MA, Messer JA, Pérez-Herrán E, Centrella PA, Alvarez-Gómez D, Clark MA, Huss S, O'Donovan GK, Ortega-Muro F, McDowell W, Castañeda P, Arico-Muendel CC, Pajk S, Rullás J, Angulo-Barturen I, Alvarez-Ruíz E, Mendoza-Losana A, Ballell Pages L, Castro-Pichel J, Evindar G..  (2014)  Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.,  57  (4): [PMID:24450589] [10.1021/jm401326j]

183. Biour M, Ben Salem C, Chazouillères O, Grangé JD, Serfaty L, Poupon R..  (2004)  [Drug-induced liver injury; fourteenth updated edition of the bibliographic database of liver injuries and related drugs].,  28  (8-9): [PMID:15646539] [10.1016/s0399-8320(04)95062-2]

184. Zhou FW, Lei HS, Fan L, Jiang L, Liu J, Peng XM, Xu XR, Chen L, Zhou CH, Zou YY, Liu CP, He ZQ, Yang DC..  (2014)  Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.,  24  (8): [PMID:24684842] [10.1016/j.bmcl.2014.03.010]

185. Shirude PS, Shandil RK, Manjunatha MR, Sadler C, Panda M, Panduga V, Reddy J, Saralaya R, Nanduri R, Ambady A, Ravishankar S, Sambandamurthy VK, Humnabadkar V, Jena LK, Suresh RS, Srivastava A, Prabhakar KR, Whiteaker J, McLaughlin RE, Sharma S, Cooper CB, Mdluli K, Butler S, Iyer PS, Narayanan S, Chatterji M..  (2014)  Lead optimization of 1,4-azaindoles as antimycobacterial agents.,  57  (13): [PMID:24874895] [10.1021/jm500571f]

186. Hameed P S, Patil V, Solapure S, Sharma U, Madhavapeddi P, Raichurkar A, Chinnapattu M, Manjrekar P, Shanbhag G, Puttur J, Shinde V, Menasinakai S, Rudrapatana S, Achar V, Awasthy D, Nandishaiah R, Humnabadkar V, Ghosh A, Narayan C, Ramya VK, Kaur P, Sharma S, Werngren J, Hoffner S, Panduga V, Kumar CN, Reddy J, Kumar K N M, Ganguly S, Bharath S, Bheemarao U, Mukherjee K, Arora U, Gaonkar S, Coulson M, Waterson D, Sambandamurthy VK, de Sousa SM..  (2014)  Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.,  57  (11): [PMID:24809953] [10.1021/jm500432n]

187. Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR..  (2014)  4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.,  57  (12): [PMID:24871036] [10.1021/jm5005978]

188. Mark Wenlock and Nicholas Tomkinson. Experimental in vitro DMPK and physicochemical data on a set of publicly disclosed compounds,  [10.6019/CHEMBL3301361]

189. Renuka J, Reddy KI, Srihari K, Jeankumar VU, Shravan M, Sridevi JP, Yogeeswari P, Babu KS, Sriram D..  (2014)  Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.,  22  (17): [PMID:25129171] [10.1016/j.bmc.2014.06.041]

190. Naik M, Ghorpade S, Jena LK, Gorai G, Narayan A, Guptha S, Sharma S, Dinesh N, Kaur P, Nandishaiah R, Bhat J, Balakrishnan G, Humnabadkar V, Ramachandran V, Naviri LK, Khadtare P, Panda M, Iyer PS, Chatterji M..  (2014)  2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.,  5  (9): [PMID:25221657] [10.1021/ml5001933]

191. Bellale E, Naik M, V B V, Ambady A, Narayan A, Ravishankar S, Ramachandran V, Kaur P, McLaughlin R, Whiteaker J, Morayya S, Guptha S, Sharma S, Raichurkar A, Awasthy D, Achar V, Vachaspati P, Bandodkar B, Panda M, Chatterji M..  (2014)  Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.,  57  (15): [PMID:24967731] [10.1021/jm500833f]

192. Hameed P S, Raichurkar A, Madhavapeddi P, Menasinakai S, Sharma S, Kaur P, Nandishaiah R, Panduga V, Reddy J, Sambandamurthy VK, Sriram D..  (2014)  Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.,  5  (7): [PMID:25050172] [10.1021/ml5001728]

193. Bobesh KA, Renuka J, Jeankumar VU, Shruti SK, Sridevi JP, Yogeeswari P, Sriram D..  (2014)  Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.,  85  [PMID:25127151] [10.1016/j.ejmech.2014.08.018]

194. Moraski GC, Oliver AG, Markley LD, Cho S, Franzblau SG, Miller MJ..  (2014)  Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.,  24  (15): [PMID:24909079] [10.1016/j.bmcl.2014.05.062]

195. Liu H, Huang J, Wang J, Wang M, Liu M, Wang B, Guo H, Lu Y..  (2014)  Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.,  86  [PMID:25218911] [10.1016/j.ejmech.2014.09.029]

196. Medapi B, Renuka J, Saxena S, Sridevi JP, Medishetti R, Kulkarni P, Yogeeswari P, Sriram D..  (2015)  Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.,  23  (9): [PMID:25801151] [10.1016/j.bmc.2015.03.004]

197. Saxena S, Samala G, Sridevi JP, Devi PB, Yogeeswari P, Sriram D..  (2015)  Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.,  92  [PMID:25585006] [10.1016/j.ejmech.2014.12.046]

198. Mirams GR, Davies MR, Brough SJ, Bridgland-Taylor MH, Cui Y, Gavaghan DJ, Abi-Gerges N..  (2014)  Prediction of Thorough QT study results using action potential simulations based on ion channel screens.,  70  [PMID:25087753] [10.1016/j.vascn.2014.07.002]

199. Wiśniowska B, Mendyk A, Fijorek K, Glinka A, Polak S..  (2012)  Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.,  32  [PMID:22761000] [10.1002/jat.2784]

200. Kramer J, Obejero-Paz CA, Myatt G, Kuryshev YA, Bruening-Wright A, Verducci JS, Brown AM..  (2013)  MICE models: superior to the HERG model in predicting Torsade de Pointes.,  3  [PMID:23812503] [10.1038/srep02100]

201. Li C, Liu JC, Li YR, Gou C, Zhang ML, Liu HY, Li XZ, Zheng CJ, Piao HR..  (2015)  Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.,  25  (15): [PMID:26048807] [10.1016/j.bmcl.2015.04.081]

202. Hameed P S, Manjrekar P, Raichurkar A, Shinde V, Puttur J, Shanbhag G, Chinnapattu M, Patil V, Rudrapatana S, Sharma S, Kumar CN, Nandishaiah R, Madhavapeddi P, Sriram D, Solapure S, Sambandamurthy VK..  (2015)  Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.,  6  (7): [PMID:26191359] [10.1021/ml500531p]

203. Huang X, Bao Y, Zhu S, Zhang X, Lan S, Wang T..  (2015)  Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.,  25  (18): [PMID:26238324] [10.1016/j.bmcl.2015.07.044]

204. Medapi B, Suryadevara P, Renuka J, Sridevi JP, Yogeeswari P, Sriram D..  (2015)  4-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.,  103  [PMID:26318054] [10.1016/j.ejmech.2015.06.032]

205. Li YR, Li C, Liu JC, Guo M, Zhang TY, Sun LP, Zheng CJ, Piao HR..  (2015)  Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.,  25  (22): [PMID:26490095] [10.1016/j.bmcl.2015.10.028]

206. Huang J, Liu H, Liu M, Zhang R, Li L, Wang B, Wang M, Wang C, Lu Y..  (2015)  Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.,  25  (22): [PMID:26476970] [10.1016/j.bmcl.2015.10.027]

207. Zhang J, Yang Q, Romero JA, Cross J, Wang B, Poutsiaka KM, Epie F, Bevan D, Wu Y, Moy T, Daniel A, Chamberlain B, Carter N, Shotwell J, Arya A, Kumar V, Silverman J, Nguyen K, Metcalf CA, Ryan D, Lippa B, Dolle RE..  (2015)  Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.,  6  (10): [PMID:26487916] [10.1021/acsmedchemlett.5b00266]

208. Bobesh KA, Renuka J, Srilakshmi RR, Yellanki S, Kulkarni P, Yogeeswari P, Sriram D..  (2016)  Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.,  24  (1): [PMID:26678175] [10.1016/j.bmc.2015.11.039]

209. Medapi B, Meda N, Kulkarni P, Yogeeswari P, Sriram D..  (2016)  Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.,  24  (4): [PMID:26787274] [10.1016/j.bmc.2016.01.011]

210. Samala G, Devi PB, Saxena S, Meda N, Yogeeswari P, Sriram D..  (2016)  Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.,  24  (6): [PMID:26867485] [10.1016/j.bmc.2016.01.059]

211. Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND..  (2016)  Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.,  26  (10): [PMID:27055939] [10.1016/j.bmcl.2016.03.106]

212. Huang J, Wang M, Wang B, Wu Z, Liu M, Feng L, Zhang J, Li X, Yang Y, Lu Y..  (2016)  Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.,  26  (9): [PMID:27020299] [10.1016/j.bmcl.2016.03.050]

213. Cross JB, Zhang J, Yang Q, Mesleh MF, Romero JA, Wang B, Bevan D, Poutsiaka KM, Epie F, Moy T, Daniel A, Shotwell J, Chamberlain B, Carter N, Andersen O, Barker J, Ryan MD, Metcalf CA, Silverman J, Nguyen K, Lippa B, Dolle RE..  (2016)  Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.,  7  (4): [PMID:27096044] [10.1021/acsmedchemlett.5b00368]

214. Reshma RS, Saxena S, Bobesh KA, Jeankumar VU, Gunda S, Yogeeswari P, Sriram D..  (2016)  Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors.,  24  (18): [PMID:27477207] [10.1016/j.bmc.2016.07.051]

215. WHO Anatomical Therapeutic Chemical Classification, 

216. British National Formulary (72nd edition), 

217. Samala G, Brindha Devi P, Saxena S, Gunda S, Yogeeswari P, Sriram D..  (2016)  Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.,  24  (21): [PMID:27667550] [10.1016/j.bmc.2016.09.012]

218. Gorityala BK, Guchhait G, Goswami S, Fernando DM, Kumar A, Zhanel GG, Schweizer F..  (2016)  Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.,  59  (18): [PMID:27524179] [10.1021/acs.jmedchem.6b00867]

219. Wei ZY, Chi KQ, Yu ZK, Liu HY, Sun LP, Zheng CJ, Piao HR..  (2016)  Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.,  26  (24): [PMID:27843112] [10.1016/j.bmcl.2016.11.001]

220. Gençer HK, Levent S, Acar Çevik U, Özkay Y, Ilgın S..  (2017)  New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.,  27  (5): [PMID:28174104] [10.1016/j.bmcl.2017.01.073]

221. Giacobbo BC, Pissinate K, Rodrigues-Junior V, Villela AD, Grams ES, Abbadi BL, Subtil FT, Sperotto N, Trindade RV, Back DF, Campos MM, Basso LA, Machado P, Santos DS..  (2017)  New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.,  126  [PMID:27914363] [10.1016/j.ejmech.2016.11.048]

222. Muharini R, Díaz A, Ebrahim W, Mándi A, Kurtán T, Rehberg N, Kalscheuer R, Hartmann R, Orfali RS, Lin W, Liu Z, Proksch P..  (2017)  Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.,  80  (1): [PMID:28075580] [10.1021/acs.jnatprod.6b00809]

223. Lyu Y, Yang X, Goswami S, Gorityala BK, Idowu T, Domalaon R, Zhanel GG, Shan A, Schweizer F..  (2017)  Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.,  60  (9): [PMID:28409644] [10.1021/acs.jmedchem.6b01742]

224. Warner DJ, Chen H, Cantin LD, Kenna JG, Stahl S, Walker CL, Noeske T..  (2012)  Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.,  40  (12): [PMID:22961681] [10.1124/dmd.112.047068]

225. Parmar A, Lakshminarayanan R, Iyer A, Mayandi V, Leng Goh ET, Lloyd DG, Chalasani MLS, Verma NK, Prior SH, Beuerman RW, Madder A, Taylor EJ, Singh I..  (2018)  Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo.,  61  (5): [PMID:29363971] [10.1021/acs.jmedchem.7b01634]

226. Chen M, Suzuki A, Thakkar S, Yu K, Hu C, Tong W..  (2016)  DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.,  21  (4): [PMID:26948801] [10.1016/j.drudis.2016.02.015]

227. Dos Santos Fernandes GF, de Souza PC, Moreno-Viguri E, Santivañez-Veliz M, Paucar R, Pérez-Silanes S, Chegaev K, Guglielmo S, Lazzarato L, Fruttero R, Man Chin C, da Silva PB, Chorilli M, Solcia MC, Ribeiro CM, Silva CSP, Marino LB, Bosquesi PL, Hunt DM, de Carvalho LPS, de Souza Costa CA, Cho SH, Wang Y, Franzblau SG, Pavan FR, Dos Santos JL..  (2017)  Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.,  60  (20): [PMID:28968083] [10.1021/acs.jmedchem.7b01332]

228. Arnold MA, Gerasyuto AI, Wang J, Du W, Gorske YJK, Arasu T, Baird J, Almstead NG, Narasimhan J, Peddi S, Ginzburg O, Lue SW, Hedrick J, Sheedy J, Lagaud G, Branstrom AA, Weetall M, Prasad JVNV, Karp GM..  (2017)  4-Hydroxy-2-pyridones: Discovery and evaluation of a novel class of antibacterial agents targeting DNA synthesis.,  27  (22): [PMID:29032026] [10.1016/j.bmcl.2017.10.006]

229. Thompson AM, Bonnet M, Lee HH, Franzblau SG, Wan B, Wong GS, Cooper CB, Denny WA..  (2017)  Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.,  8  (12): [PMID:29259747] [10.1021/acsmedchemlett.7b00356]

230. Cvijetić IN, Verbić TŽ, Ernesto de Resende P, Stapleton P, Gibbons S, Juranić IO, Drakulić BJ, Zloh M..  (2018)  Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.,  143  [PMID:29133041] [10.1016/j.ejmech.2017.10.045]

231. Yan X, Lv Z, Wen J, Zhao S, Xu Z..  (2018)  Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities.,  143  [PMID:29227930] [10.1016/j.ejmech.2017.11.090]

232. Reshma RS, Jeankumar VU, Kapoor N, Saxena S, Bobesh KA, Vachaspathy AR, Kolattukudy PE, Sriram D..  (2017)  Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.,  25  (10): [PMID:28389113] [10.1016/j.bmc.2017.03.053]

233. Malapati P, Siva Krishna V, Nallangi R, Meda N, Reshma Srilakshmi R, Sriram D..  (2018)  Lead identification and optimization of bacterial glutamate racemase inhibitors.,  26  (1): [PMID:29239770] [10.1016/j.bmc.2017.11.031]

234. Gerasyuto AI, Arnold MA, Wang J, Chen G, Zhang X, Smith S, Woll MG, Baird J, Zhang N, Almstead NG, Narasimhan J, Peddi S, Dumble M, Sheedy J, Weetall M, Branstrom AA, Prasad JVN, Karp GM..  (2018)  Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.,  61  (10): [PMID:29727185] [10.1021/acs.jmedchem.8b00114]

235. Cleghorn LAT, Ray PC, Odingo J, Kumar A, Wescott H, Korkegian A, Masquelin T, Lopez Moure A, Wilson C, Davis S, Huggett M, Turner P, Smith A, Epemolu O, Zuccotto F, Riley J, Scullion P, Shishikura Y, Ferguson L, Rullas J, Guijarro L, Read KD, Green SR, Hipskind P, Parish T, Wyatt PG..  (2018)  Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.,  61  (15): [PMID:29944372] [10.1021/acs.jmedchem.8b00172]

236. Zhang TY, Yu ZK, Jin XJ, Li MY, Sun LP, Zheng CJ, Piao HR..  (2018)  Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.,  28  (9): [PMID:29588213] [10.1016/j.bmcl.2018.03.037]

237. Fan YL, Wu JB, Cheng XW, Zhang FZ, Feng LS..  (2018)  Fluoroquinolone derivatives and their anti-tubercular activities.,  146  [PMID:29407980] [10.1016/j.ejmech.2018.01.080]

238. Asfaw H, Wetzlar T, Martinez-Martinez MS, Imming P..  (2018)  An efficient synthetic route for preparation of antimycobacterial wollamides and evaluation of their in vitro and in vivo efficacy.,  28  (17): [PMID:30031620] [10.1016/j.bmcl.2018.07.021]

239. Odagiri T, Inagaki H, Nagamochi M, Kitamura T, Komoriya S, Takahashi H..  (2018)  Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.,  61  (16): [PMID:30063826] [10.1021/acs.jmedchem.8b00644]

240. McGarry DH, Cooper IR, Walker R, Warrilow CE, Pichowicz M, Ratcliffe AJ, Salisbury AM, Savage VJ, Moyo E, Maclean J, Smith A, Charrier C, Stokes NR, Lindsay DM, Kerr WJ..  (2018)  Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.,  28  (17): [PMID:30122228] [10.1016/j.bmcl.2018.05.049]

241. Malapati P, Krishna VS, Nallangi R, Srilakshmi RR, Sriram D..  (2018)  Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.,  145  [PMID:29310027] [10.1016/j.ejmech.2017.12.088]

242. Poce G, Cocozza M, Alfonso S, Consalvi S, Venditti G, Fernandez-Menendez R, Bates RH, Barros Aguirre D, Ballell L, De Logu A, Vistoli G, Biava M..  (2018)  In vivo potent BM635 analogue with improved drug-like properties.,  145  [PMID:29335214] [10.1016/j.ejmech.2017.12.075]

243. Lu X, Hu X, Liu Z, Zhang T, Wang R, Wan B, Franzblau SG, You Q..  (2017)  Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant Mycobacterium tuberculosis.,  8  (6): [PMID:30108841] [10.1039/C7MD00146K]

244. Unpublished dataset, 

245. Franck Touret, Magali Gilles, Karine Barral, Antoine Nougairède, Etienne Decroly, Xavier de Lamballerie, Bruno Coutard.  (2020)  In vitro screening of a FDA approved chemical library reveals potential inhibitors of SARS-CoV-2 replication,  [10.1101/2020.04.03.023846]

246. Katie Heiser, Peter F. McLean, Chadwick T. Davis, Ben Fogelson, Hannah B. Gordon, Pamela Jacobson, Brett Hurst, Ben Miller, Ronald W. Alfa, Berton A. Earnshaw, Mason L. Victors, Yolanda T. Chong, Imran S. Haque, Adeline S. Low, Christopher C. Gibson.  (2020)  Identification of potential treatments for COVID-19 through artificial intelligence-enabled phenomic analysis of human cells infected with SARS-CoV-2,  [10.1101/2020.04.21.054387]

247. Poce G, Consalvi S, Venditti G, Alfonso S, Desideri N, Fernandez-Menendez R, Bates RH, Ballell L, Barros Aguirre D, Rullas J, De Logu A, Gardner M, Ioerger TR, Rubin EJ, Biava M..  (2019)  Novel Pyrazole-Containing Compounds Active against Mycobacterium tuberculosis.,  10  (10): [PMID:31620228] [10.1021/acsmedchemlett.9b00204]

248. Shruthi TG, Eswaran S, Shivarudraiah P, Narayanan S, Subramanian S..  (2019)  Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.,  29  (1): [PMID:30448235] [10.1016/j.bmcl.2018.11.002]

249. Zhang TY, Zheng CJ, Wu J, Sun LP, Piao HR..  (2019)  Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.,  29  (9): [PMID:30842033] [10.1016/j.bmcl.2019.02.033]

250. Bangalore PK, Vagolu SK, Bollikanda RK, Veeragoni DK, Choudante PC, Misra S, Sriram D, Sridhar B, Kantevari S..  (2020)  Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents.,  83  (1): [PMID:31858800] [10.1021/acs.jnatprod.9b00475]

251. Liu H, Sun D, Du H, Zheng C, Li J, Piao H, Li J, Sun L..  (2019)  Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.,  172  [PMID:30978561] [10.1016/j.ejmech.2019.03.059]

252. Pham TDM, Ziora ZM, Blaskovich MAT..  (2019)  Quinolone antibiotics.,  10  (10): [PMID:31803393] [10.1039/C9MD00120D]

253. Cappoen D, Torfs E, Meiresonne T, Claes P, Semina E, Holvoet F, de Macedo MB, Cools F, Piller T, Matheeussen A, Van Calster K, Caljon G, Delputte P, Maes L, Neyrolles O, De Kimpe N, Mangelinckx S, Cos P..  (2019)  The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.,  181  [PMID:31376569] [10.1016/j.ejmech.2019.07.052]

254. Gao F, Chen Z, Ma L, Fan Y, Chen L, Lu G..  (2019)  Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.,  180  [PMID:31352245] [10.1016/j.ejmech.2019.07.057]

255. Xu Z, Zhao SJ, Lv ZS, Gao F, Wang Y, Zhang F, Bai L, Deng JL..  (2019)  Fluoroquinolone-isatin hybrids and their biological activities.,  162  [PMID:30453247] [10.1016/j.ejmech.2018.11.032]

256. Zhang W, Lun S, Liu LL, Xiao S, Duan G, Gunosewoyo H, Yang F, Tang J, Bishai WR, Yu LF..  (2019)  Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.,  62  (7): [PMID:30875203] [10.1021/acs.jmedchem.9b00010]

257. Fedorowicz J, Sączewski J, Konopacka A, Waleron K, Lejnowski D, Ciura K, Tomašič T, Skok Ž, Savijoki K, Morawska M, Gilbert-Girard S, Fallarero A..  (2019)  Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.,  179  [PMID:31279292] [10.1016/j.ejmech.2019.06.071]

258. Song M, Wang S, Wang Z, Fu Z, Zhou S, Cheng H, Liang Z, Deng X..  (2019)  Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.,  166  [PMID:30685534] [10.1016/j.ejmech.2019.01.038]

259. Fumagalli F, de Melo SMG, Ribeiro CM, Solcia MC, Pavan FR, da Silva Emery F..  (2019)  Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.,  29  (8): [PMID:30803803] [10.1016/j.bmcl.2019.02.019]

260. Borthwick JA, Alemparte C, Wall I, Whitehurst BC, Argyrou A, Burley G, de Dios-Anton P, Guijarro L, Monteiro MC, Ortega F, Suckling CJ, Pichel JC, Cacho M, Young RJ..  (2020)  Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity.,  63  (5): [PMID:31922409] [10.1021/acs.jmedchem.9b01561]

261. Mayandi V, Xi Q, Leng Goh ET, Koh SK, Jie Toh TY, Barathi VA, Urf Turabe Fazil MH, Somaraju Chalasani ML, Varadarajan J, Jeng Ting DS, Beuerman RW, Chan LW, Agrawal R, Sebastian Barkham TM, Zhou L, Verma NK, Lakshminarayanan R..  (2020)  Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.,  63  (7): [PMID:32175733] [10.1021/acs.jmedchem.9b01846]

262. Balabon O, Pitta E, Rogacki MK, Meiler E, Casanueva R, Guijarro L, Huss S, Lopez-Roman EM, Santos-Villarejo Á, Augustyns K, Ballell L, Aguirre DB, Bates RH, Cunningham F, Cacho M, Van der Veken P..  (2020)  Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.,  63  (10): [PMID:32342688] [10.1021/acs.jmedchem.0c00107]

263. Meier D, Hernández MV, van Geelen L, Muharini R, Proksch P, Bandow JE, Kalscheuer R..  (2019)  The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria.,  27  (23): [PMID:31648878] [10.1016/j.bmc.2019.115151]

264. Ma Z, Lynch AS..  (2016)  Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.,  59  (14): [PMID:27336583] [10.1021/acs.jmedchem.6b00485]

265. Ebrahim W, El-Neketi M, Lewald LI, Orfali RS, Lin W, Rehberg N, Kalscheuer R, Daletos G, Proksch P..  (2016)  Metabolites from the Fungal Endophyte Aspergillus austroafricanus in Axenic Culture and in Fungal-Bacterial Mixed Cultures.,  79  (4): [PMID:27070198] [10.1021/acs.jnatprod.5b00975]

266. Maria Kuzikov, Elisa Costanzi, Jeanette Reinshagen, Francesca Esposito, Laura Vangeel, Markus Wolf, Bernhard Ellinger, Carsten Claussen, Gerd Geisslinger, Angela Corona, Daniela Iaconis, Carmine Talarico, Candida Manelfi, Rolando Cannalire, Giulia Rossetti, Jonas Gossen, Simone Albani, Francesco Musiani, Katja Herzog, Yang Ye, Barbara Giabbai, Nicola Demitri, Dirk Jochmans, Steven De Jonghe, Jasper Rymenants, Vincenzo Summa, Enzo Tramontano, Andrea R. Beccari, Pieter Leyssen, Paola Storici, Johan Neyts, Philip Gribbon, and Andrea Zaliani.  (2020)  Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen,  [10.6019/CHEMBL4495564]

267. Andrea Zaliani, Laura Vangeel, Jeanette Reinshagen, Daniela Iaconis, Maria Kuzikov, Oliver Keminer, Markus Wolf, Bernhard Ellinger, Francesca Esposito, Angela Corona, Enzo Tramontano, Candida Manelfi, Katja Herzog, Dirk Jochmans, Steven De Jonghe, Winston Chiu, Thibault Francken, Joost Schepers, Caroline Collard, Kayvan Abbasi, Carsten Claussen , Vincenzo Summa, Andrea R. Beccari, Johan Neyts, Philip Gribbon and Pieter Leyssen.  (2020)  Cytopathic SARS-Cov2 screening on VERO-E6 cells in a large repurposing effort,  [10.6019/CHEMBL4495565]

268. Picconi P, Hind CK, Nahar KS, Jamshidi S, Di Maggio L, Saeed N, Evans B, Solomons J, Wand ME, Sutton JM, Rahman KM..  (2020)  New Broad-Spectrum Antibiotics Containing a Pyrrolobenzodiazepine Ring with Activity against Multidrug-Resistant Gram-Negative Bacteria.,  63  (13): [PMID:32515951] [10.1021/acs.jmedchem.0c00328]

269. Touitou M, Manetti F, Ribeiro CM, Pavan FR, Scalacci N, Zrebna K, Begum N, Semenya D, Gupta A, Bhakta S, McHugh TD, Senderowitz H, Kyriazi M, Castagnolo D..  (2020)  Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria.,  11  (5): [PMID:32435364] [10.1021/acsmedchemlett.9b00515]

270. Dana S, Valissery P, Kumar S, Gurung SK, Mondal N, Dhar SK, Mukhopadhyay P..  (2020)  Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity.,  11  (7): [PMID:32676153] [10.1021/acsmedchemlett.0c00196]

271. Ellen Van Damme.  (2021)  Screening of ~5500 FDA-approved drugs and clinical candidates for anti-SARS-CoV-2 activity,  [10.6019/CHEMBL4651402]

272. Roth L,Gotsbacher MP,Codd R.  (2020)  Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.,  63  (20.0): [PMID:32940035] [10.1021/acs.jmedchem.0c01541]

273. Berry, Liam, Domalaon, Ronald, Brizuela, Marc, Zhanel, George G., Schweizer, Frank.  (2019)  Polybasic peptide-levofloxacin conjugates potentiate fluoroquinolones and other classes of antibiotics against multidrug-resistant Gram-negative bacteria,  10  (4): [PMID:31057731] [10.1039/c9md00051h]

274. Sirim MM,Krishna VS,Sriram D,Unsal Tan O.  (2020)  Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.,  188  [PMID:31893548] [10.1016/j.ejmech.2019.112010]

275. Krishna VS,Zheng S,Rekha EM,Nallangi R,Sai Prasad DV,George SE,Guddat LW,Sriram D.  (2020)  Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.,  193  [PMID:32171154] [10.1016/j.ejmech.2020.112178]

276. Rehberg N,Sommer GA,Drießen D,Kruppa M,Adeniyi ET,Chen S,Wang L,Wolf K,Tasch BOA,Ioerger TR,Zhu K,Müller TJJ,Kalscheuer R.  (2020)  Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial In Vitro and In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus.,  63  (21): [PMID:33103423] [10.1021/acs.jmedchem.0c00826]

277. Xu Z.  (2020)  1,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).,  206  [PMID:32795773] [10.1016/j.ejmech.2020.112686]

278. Kirk R,Betson M,Bingham M,Doyle P,Harvey R,Huxley A,Moat J,Pesnot T,Tait M,Hallworth S,Nelson G.  (2020)  Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.,  30  (20): [PMID:32799032] [10.1016/j.bmcl.2020.127428]

279. Mohammed AAM,Suaifan GARY,Shehadeh MB,Okechukwu PN.  (2020)  Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.,  202  [PMID:32623216] [10.1016/j.ejmech.2020.112513]

280. Coulibaly S,Cimino M,Ouattara M,Lecoutey C,Buchieri MV,Alonso-Rodriguez N,Briffotaux J,Mornico D,Gicquel B,Rochais C,Dallemagne P.  (2020)  Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.,  207  [PMID:32950907] [10.1016/j.ejmech.2020.112821]

281. Bernhard Ellinger, Justus Dick, Vanessa Lage-Rupprecht, Bruce Schultz, Andrea Zaliani, Marcin Namysl, Stephan Gebel, Ole Pless, Jeanette Reinshagen, Christian Ebeling, Alexander Esser, Marc Jacobs, Carsten Claussen, and Martin Hofmann-Apitius.  (2021)  HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators,  [10.6019/CHEMBL4808148]

282. Lapointe G, Skepper CK, Holder LM, Armstrong D, Bellamacina C, Blais J, Bussiere D, Bian J, Cepura C, Chan H, Dean CR, De Pascale G, Dhumale B, Fisher LM, Fulsunder M, Kantariya B, Kim J, King S, Kossy L, Kulkarni U, Lakshman J, Leeds JA, Ling X, Lvov A, Ma S, Malekar S, McKenney D, Mergo W, Metzger L, Mhaske K, Moser HE, Mostafavi M, Namballa S, Noeske J, Osborne C, Patel A, Patel D, Patel T, Piechon P, Polyakov V, Prajapati K, Prosen KR, Reck F, Richie DL, Sanderson MR, Satasia S, Savani B, Selvarajah J, Sethuraman V, Shu W, Tashiro K, Thompson KV, Vaarla K, Vala L, Veselkov DA, Vo J, Vora B, Wagner T, Wedel L, Williams SL, Yendluri S, Yue Q, Yifru A, Zhang Y, Rivkin A..  (2021)  Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.,  64  (9.0): [PMID:33929852] [10.1021/acs.jmedchem.1c00375]

283. De Ruysscher D, Pang L, Lenders SMG, Cappoen D, Cos P, Rozenski J, Strelkov SV, Weeks SD, Van Aerschot A..  (2021)  Synthesis and structure-activity studies of novel anhydrohexitol-based Leucyl-tRNA synthetase inhibitors.,  211  [PMID:33248851] [10.1016/j.ejmech.2020.113021]

284. Semenya D, Touitou M, Ribeiro CM, Pavan FR, Pisano L, Singh V, Chibale K, Bano G, Toscani A, Manetti F, Gianibbi B, Castagnolo D..  (2022)  Structural Rigidification of N-Aryl-pyrroles into Indoles Active against Intracellular and Drug-Resistant Mycobacteria.,  13  (1.0): [PMID:35059125] [10.1021/acsmedchemlett.1c00431]

285. Beuchel A, Robaa D, Negatu DA, Madani A, Alvarez N, Zimmerman MD, Richter A, Mann L, Hoenke S, Csuk R, Dick T, Imming P..  (2022)  Structure-Activity Relationship of Anti-Mycobacterium abscessus Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors.,  13  (3.0): [PMID:35300094] [10.1021/acsmedchemlett.1c00549]

286. Huang Z, Luo W, Xu D, Guo F, Yang M, Zhu Y, Shen L, Chen S, Tang D, Li L, Li Y, Wang B, Franzblau SG, Ding CZ..  (2022)  Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.,  71  [PMID:35636648] [10.1016/j.bmcl.2022.128824]

287. Luo W, Huang Z, Xu D, Yang M, Zhu Y, Shen L, Chen S, Tao X, Bin W, Hu Y, Franzblau SG, Jiang N, Wei Y, Wei X, Ding CZ..  (2022)  Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.,  72  [PMID:35777718] [10.1016/j.bmcl.2022.128871]

288. Semenya D, Touitou M, Masci D, Ribeiro CM, Pavan FR, Dos Santos Fernandes GF, Gianibbi B, Manetti F, Castagnolo D..  (2022)  Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.,  237  [PMID:35486992] [10.1016/j.ejmech.2022.114404]

289. Perveen S, Kumari D, Singh K, Sharma R..  (2022)  Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.,  229  [PMID:34973508] [10.1016/j.ejmech.2021.114066]

290. Sadowski E, Bercot B, Chauffour A, Gomez C, Varon E, Mainardis M, Sougakoff W, Mayer C, Sachon E, Anquetin G, Aubry A..  (2022)  Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.,  55  [PMID:34774742] [10.1016/j.bmcl.2021.128450]

291. Peek J, Koirala B, Brady SF..  (2022)  Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.,  57  [PMID:34861348] [10.1016/j.bmcl.2021.128484]

292. Bhawsar S, Joshi S, Deshpande P, Yeole R, Bhagwat S, Patel M..  (2022)  WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.,  63  [PMID:35276361] [10.1016/j.bmcl.2022.128665]

293. Panciera M, Lence E, Rodríguez Á, Gracia B, Aínsa JA, Marco-Marín C, Rubio V, Duarte Correia CR, González-Bello C..  (2022)  Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme.,  232  [PMID:35219949] [10.1016/j.ejmech.2022.114206]

294. Govender P, Müller R, Singh K, Reddy V, Eyermann CJ, Fienberg S, Ghorpade SR, Koekemoer L, Myrick A, Schnappinger D, Engelhart C, Meshanni J, Byl JAW, Osheroff N, Singh V, Chibale K, Basarab GS..  (2022)  Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.,  65  (9.0): [PMID:35500229] [10.1021/acs.jmedchem.2c00266]

295. Yuan Y, Jin W, Nazir Y, Fercher C, Blaskovich MAT, Cooper MA, Barnard RT, Ziora ZM..  (2020)  Tyrosinase inhibitors as potential antibacterial agents.,  187  [PMID:31810785] [10.1016/j.ejmech.2019.111892]

296. Verma R, Verma SK, Rakesh KP, Girish YR, Ashrafizadeh M, Sharath Kumar KS, Rangappa KS..  (2021)  Pyrazole-based analogs as potential antibacterial agents against methicillin-resistance staphylococcus aureus (MRSA) and its SAR elucidation.,  212  [PMID:33395624] [10.1016/j.ejmech.2020.113134]

297. Jia Y, Zhao L..  (2021)  The antibacterial activity of fluoroquinolone derivatives: An update (2018-2021).,  224  [PMID:34365130] [10.1016/j.ejmech.2021.113741]

298. Fan YL, Cheng XW, Wu JB, Liu M, Zhang FZ, Xu Z, Feng LS..  (2018)  Antiplasmodial and antimalarial activities of quinolone derivatives: An overview.,  146  [PMID:29360043] [10.1016/j.ejmech.2018.01.039]

299. Gao C, Fan YL, Zhao F, Ren QC, Wu X, Chang L, Gao F..  (2018)  Quinolone derivatives and their activities against methicillin-resistant Staphylococcus aureus (MRSA).,  157  [PMID:30179746] [10.1016/j.ejmech.2018.08.061]

300. Gao F, Wang P, Yang H, Miao Q, Ma L, Lu G..  (2018)  Recent developments of quinolone-based derivatives and their activities against Escherichia coli.,  157  [PMID:30193220] [10.1016/j.ejmech.2018.08.095]

301. Durcik M, Cotman AE, Toplak Ž, Možina Š, Skok Ž, Szili PE, Czikkely M, Maharramov E, Vu TH, Piras MV, Zidar N, Ilaš J, Zega A, Trontelj J, Pardo LA, Hughes D, Huseby D, Berruga-Fernández T, Cao S, Simoff I, Svensson R, Korol SV, Jin Z, Vicente F, Ramos MC, Mundy JEA, Maxwell A, Stevenson CEM, Lawson DM, Glinghammar B, Sjöström E, Bohlin M, Oreskär J, Alvér S, Janssen GV, Sterk GJ, Kikelj D, Pal C, Tomašič T, Peterlin Mašič L..  (2023)  New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus.,  66  (6): [PMID:36877255] [10.1021/acs.jmedchem.2c01905]

302. Mishra SK, Tripathi G, Kishore N, Singh RK, Singh A, Tiwari VK..  (2017)  Drug development against tuberculosis: Impact of alkaloids.,  137  [PMID:28628823] [10.1016/j.ejmech.2017.06.005]

303. Sutherland JJ, Yonchev D, Fekete A, Urban L..  (2023)  A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.,  14  (1): [PMID:37468498] [10.1038/s41467-023-40064-9]

Source

Source(9):

• Scientific Literature
• Clinical Candidates
• USP Dictionary of USAN and International Drug Names
• AstraZeneca Deposited Data
• WHO Anatomical Therapeutic Chemical Classification
• British National Formulary
• SARS-CoV-2 Screening Data 2020-21
• IMI-CARE SARS-CoV-2 Data
• Fraunhofer HDAC6