| 1. Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discenza L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN.. (2008) Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes., 51 (5): [PMID:18260618] [10.1021/jm701272q] |
| 2. Washburn WN.. (2009) Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2., 52 (7): [PMID:19243175] [10.1021/jm8013019] |
| 3. Xu B, Lv B, Feng Y, Xu G, Du J, Welihinda A, Sheng Z, Seed B, Chen Y.. (2009) O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors., 19 (19): [PMID:19700318] [10.1016/j.bmcl.2009.08.030] |
| 4. Goodwin NC, Mabon R, Harrison BA, Shadoan MK, Almstead ZY, Xie Y, Healy J, Buhring LM, DaCosta CM, Bardenhagen J, Mseeh F, Liu Q, Nouraldeen A, Wilson AG, Kimball SD, Powell DR, Rawlins DB.. (2009) Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes., 52 (20): [PMID:19785435] [10.1021/jm900951n] |
| 5. Lv B, Xu B, Feng Y, Peng K, Xu G, Du J, Zhang L, Zhang W, Zhang T, Zhu L, Ding H, Sheng Z, Welihinda A, Seed B, Chen Y.. (2009) Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors., 19 (24): [PMID:19896374] [10.1016/j.bmcl.2009.10.088] |
| 6. Lee J, Lee SH, Seo HJ, Son EJ, Lee SH, Jung ME, Lee M, Han HK, Kim J, Kang J, Lee J.. (2010) Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners., 18 (6): [PMID:20181486] [10.1016/j.bmc.2010.01.073] |
| 7. Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T.. (2010) C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization., 20 (5): [PMID:20149653] [10.1016/j.bmcl.2010.01.075] |
| 8. Kakinuma H, Oi T, Hashimoto-Tsuchiya Y, Arai M, Kawakita Y, Fukasawa Y, Iida I, Hagima N, Takeuchi H, Chino Y, Asami J, Okumura-Kitajima L, Io F, Yamamoto D, Miyata N, Takahashi T, Uchida S, Yamamoto K.. (2010) (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment., 53 (8): [PMID:20302302] [10.1021/jm901893x] |
| 9. Kim MJ, Lee J, Kang SY, Lee SH, Son EJ, Jung ME, Lee SH, Song KS, Lee M, Han HK, Kim J, Lee J.. (2010) Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners., 20 (11): [PMID:20434909] [10.1016/j.bmcl.2010.04.006] |
| 10. Xu B, Feng Y, Lv B, Xu G, Zhang L, Du J, Peng K, Xu M, Dong J, Zhang W, Zhang T, Zhu L, Ding H, Sheng Z, Welihinda A, Seed B, Chen Y.. (2010) ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors., 18 (12): [PMID:20576578] [10.1016/j.bmc.2010.04.088] |
| 11. Kang SY, Song KS, Lee J, Lee SH, Lee J.. (2010) Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors., 18 (16): [PMID:20637636] [10.1016/j.bmc.2010.06.076] |
| 12. Lee J, Kim JY, Choi J, Lee SH, Kim J, Lee J.. (2010) Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors., 20 (23): [PMID:20952196] [10.1016/j.bmcl.2010.09.103] |
| 13. Park EJ, Kong Y, Lee JS, Lee SH, Lee J.. (2011) Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2., 21 (2): [PMID:21193308] [10.1016/j.bmcl.2010.11.115] |
| 14. Yao CH, Song JS, Chen CT, Yeh TK, Hung MS, Chang CC, Liu YW, Yuan MC, Hsieh CJ, Huang CY, Wang MH, Chiu CH, Hsieh TC, Wu SH, Hsiao WC, Chu KF, Tsai CH, Chao YS, Lee JC.. (2011) Discovery of novel N-β-D-xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes., 54 (1): [PMID:21128592] [10.1021/jm101072y] |
| 15. Song KS, Lee SH, Kim MJ, Seo HJ, Lee J, Lee SH, Jung ME, Son EJ, Lee M, Kim J, Lee J.. (2011) Synthesis and SAR of Thiazolylmethylphenyl Glucoside as Novel C-Aryl Glucoside SGLT2 Inhibitors., 2 (2): [PMID:24900297] [10.1021/ml100256c] |
| 16. Li AR, Zhang J, Greenberg J, Lee T, Liu J.. (2011) Discovery of non-glucoside SGLT2 inhibitors., 21 (8): [PMID:21398124] [10.1016/j.bmcl.2011.02.056] |
| 17. Kang SY, Kim MJ, Lee JS, Lee J.. (2011) Glucosides with cyclic diarylpolynoid as novel C-aryl glucoside SGLT2 inhibitors., 21 (12): [PMID:21592794] [10.1016/j.bmcl.2011.04.063] |
| 18. Du X, Lizarzaburu M, Turcotte S, Lee T, Greenberg J, Shan B, Fan P, Ling Y, Medina JC, Houze J.. (2011) Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors., 21 (12): [PMID:21565497] [10.1016/j.bmcl.2011.04.053] |
| 19. Lee SH, Kim MJ, Lee SH, Kim J, Park HJ, Lee J.. (2011) Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors., 46 (7): [PMID:21514014] [10.1016/j.ejmech.2011.03.052] |
| 20. Xu B, Feng Y, Cheng H, Song Y, Lv B, Wu Y, Wang C, Li S, Xu M, Du J, Peng K, Dong J, Zhang W, Zhang T, Zhu L, Ding H, Sheng Z, Welihinda A, Roberge JY, Seed B, Chen Y.. (2011) C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes., 21 (15): [PMID:21737266] [10.1016/j.bmcl.2011.06.032] |
| 21. Kim MJ, Lee SH, Park SO, Kang H, Lee JS, Lee KN, Jung ME, Kim J, Lee J.. (2011) Novel macrocyclic C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents., 19 (18): [PMID:21868239] [10.1016/j.bmc.2011.07.045] |
| 22. Lee SH, Song KS, Kim JY, Kang M, Lee JS, Cho SH, Park HJ, Kim J, Lee J.. (2011) Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents., 19 (19): [PMID:21906953] [10.1016/j.bmc.2011.08.014] |
| 23. Li LT, Zhou LF, Li YJ, Huang J, Liu RH, Wang B, Wang P.. (2012) Facile synthesis of 1,2,3-triazole analogs of SGLT2 inhibitors by 'click chemistry'., 22 (1): [PMID:22079028] [10.1016/j.bmcl.2011.10.062] |
| 24. Ohtake Y, Sato T, Matsuoka H, Kobayashi T, Nishimoto M, Taka N, Takano K, Yamamoto K, Ohmori M, Higuchi T, Murakata M, Morikawa K, Shimma N, Suzuki M, Hagita H, Ozawa K, Yamaguchi K, Kato M, Ikeda S.. (2012) C-Aryl 5a-carba-β-d-glucopyranosides as novel sodium glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes., 20 (13): [PMID:22652255] [10.1016/j.bmc.2012.04.053] |
| 25. Yao CH, Song JS, Chen CT, Yeh TK, Hsieh TC, Wu SH, Huang CY, Huang YL, Wang MH, Liu YW, Tsai CH, Kumar CR, Lee JC.. (2012) Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors., 55 [PMID:22818040] [10.1016/j.ejmech.2012.06.053] |
| 26. USP Dictionary of USAN and International Names (2010 edition) and USAN registrations 2007-date, |
| 27. Ohtake Y, Sato T, Kobayashi T, Nishimoto M, Taka N, Takano K, Yamamoto K, Ohmori M, Yamaguchi M, Takami K, Yeu SY, Ahn KH, Matsuoka H, Morikawa K, Suzuki M, Hagita H, Ozawa K, Yamaguchi K, Kato M, Ikeda S.. (2012) Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes., 55 (17): [PMID:22889351] [10.1021/jm300884k] |
| 28. Putapatri SR, Kanwal A, Banerjee SK, Kantevari S.. (2014) Synthesis of novel l-rhamnose derived acyclic C-nucleosides with substituted 1,2,3-triazole core as potent sodium-glucose co-transporter (SGLT) inhibitors., 24 (6): [PMID:24556379] [10.1016/j.bmcl.2014.01.077] |
| 29. Xu G, Lv B, Roberge JY, Xu B, Du J, Dong J, Chen Y, Peng K, Zhang L, Tang X, Feng Y, Xu M, Fu W, Zhang W, Zhu L, Deng Z, Sheng Z, Welihinda A, Sun X.. (2014) Design, synthesis, and biological evaluation of deuterated C-aryl glycoside as a potent and long-acting renal sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes., 57 (4): [PMID:24456245] [10.1021/jm401780b] |
| 30. Guo C, Hu M, DeOrazio RJ, Usyatinsky A, Fitzpatrick K, Zhang Z, Maeng JH, Kitchen DB, Tom S, Luche M, Khmelnitsky Y, Mhyre AJ, Guzzo PR, Liu S.. (2014) The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties., 22 (13): [PMID:24842618] [10.1016/j.bmc.2014.04.036] |
| 31. Zhou J, Xu J, Huang Z, Wang M.. (2015) Transporter-mediated tissue targeting of therapeutic molecules in drug discovery., 25 (5): [PMID:25650254] [10.1016/j.bmcl.2015.01.016] |
| 32. (2015) Aryl glycoside compound, preparation method and use thereof, |
| 33. Pan X, Huan Y, Shen Z, Liu Z.. (2016) Synthesis and biological evaluation of novel tetrahydroisoquinoline-C-aryl glucosides as SGLT2 inhibitors for the treatment of type 2 diabetes., 114 [PMID:26974378] [10.1016/j.ejmech.2016.02.053] |
| 34. WHO Anatomical Therapeutic Chemical Classification, |
| 35. British National Formulary (72nd edition), |
| 36. Jesus AR, Vila-Viçosa D, Machuqueiro M, Marques AP, Dore TM, Rauter AP.. (2017) Targeting Type 2 Diabetes with C-Glucosyl Dihydrochalcones as Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitors: Synthesis and Biological Evaluation., 60 (2): [PMID:28098449] [10.1021/acs.jmedchem.6b01134] |
| 37. Li Y, Shi Z, Chen L, Zheng S, Li S, Xu B, Liu Z, Liu J, Deng C, Ye F.. (2017) Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes., 60 (10): [PMID:28447791] [10.1021/acs.jmedchem.6b01818] |
| 38. Zhao X, Sun B, Zheng H, Liu J, Qian L, Wang X, Lou H.. (2018) Synthesis and biological evaluation of 6-hydroxyl C-aryl glucoside derivatives as novel sodium glucose co-transporter 2 (SGLT2) inhibitors., 28 (12): [PMID:29764742] [10.1016/j.bmcl.2018.04.070] |
| 39. Yuan MC, Yeh TK, Chen CT, Song JS, Huang YC, Hsieh TC, Huang CY, Huang YL, Wang MH, Wu SH, Yao CH, Chao YS, Lee JC.. (2018) Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2., 143 [PMID:29216560] [10.1016/j.ejmech.2017.11.019] |
| 40. Li Z, Xu X, Deng L, Liao R, Liang R, Zhang B, Zhang L.. (2018) Design, synthesis and biological evaluation of nitric oxide releasing derivatives of dapagliflozin as potential anti-diabetic and anti-thrombotic agents., 26 (14): [PMID:29954682] [10.1016/j.bmc.2018.06.017] |
| 41. Unpublished dataset, |
| 42. Bernhard Ellinger, Denisa Bojkova, Andrea Zaliani, Jindrich Cinatl, Carsten Claussen, Sandra Westhaus, Jeanette Reinshagen, Maria Kuzikov, Markus Wolf, Gerd Geisslinger, Philip Gribbon, Sandra Ciesek. (2020) Identification of inhibitors of SARS-CoV-2 in-vitro cellular toxicity in human (Caco-2) cells using a large scale drug repurposing collection, [10.21203/rs.3.rs-23951/v1] |
| 43. 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] |
| 44. Haider K, Pathak A, Rohilla A, Haider MR, Ahmad K, Yar MS.. (2019) Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review., 184 [PMID:31630053] [10.1016/j.ejmech.2019.111773] |
| 45. Romero FA, Jones CT, Xu Y, Fenaux M, Halcomb RL.. (2020) The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease., 63 (10): [PMID:31930920] [10.1021/acs.jmedchem.9b01701] |
| 46. Wang Y, Lou Y, Wang J, Li D, Chen H, Zheng T, Xia C, Song X, Dong T, Li J, Li J, Liu H.. (2019) Design, synthesis and biological evaluation of 6-deoxy O-spiroketal C-arylglucosides as novel renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes., 180 [PMID:31325786] [10.1016/j.ejmech.2019.07.032] |
| 47. 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] |
| 48. 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] |
| 49. 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] |
| 50. 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] |
| 51. Ellen Van Damme. (2021) Screening of ~5500 FDA-approved drugs and clinical candidates for anti-SARS-CoV-2 activity, [10.6019/CHEMBL4651402] |
| 52. 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] |
| 53. Ferreira MA, Azevedo H, Mascarello A, Segretti ND, Russo E, Russo V, Guimarães CRW.. (2021) Discovery of ACH-000143: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats., 64 (4.0): [PMID:33626870] [10.1021/acs.jmedchem.0c00627] |
| 54. Kong YK, Song KS, Jung ME, Kang M, Kim HJ, Kim MJ.. (2022) Discovery of GCC5694A: A potent and selective sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes., 56 [PMID:34813882] [10.1016/j.bmcl.2021.128466] |
| 55. Zhang D, Wei C, Hop CECA, Wright MR, Hu M, Lai Y, Khojasteh SC, Humphreys WG.. (2021) Intestinal Excretion, Intestinal Recirculation, and Renal Tubule Reabsorption Are Underappreciated Mechanisms That Drive the Distribution and Pharmacokinetic Behavior of Small Molecule Drugs., 64 (11.0): [PMID:34010555] [10.1021/acs.jmedchem.0c01720] |
| 56. Wu YJ, Meanwell NA.. (2021) Geminal Diheteroatomic Motifs: Some Applications of Acetals, Ketals, and Their Sulfur and Nitrogen Homologues in Medicinal Chemistry and Drug Design., 64 (14.0): [PMID:34213340] [10.1021/acs.jmedchem.1c00790] |
| 57. 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] |
