Document Report Card

ID: ALA1141145

Journal: J Med Chem

Title: A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.

Authors: 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.

Abstract: There is an urgent medical need for novel antibacterial agents to treat hospital infections, specially those caused by multidrug-resistant Gram-positive pathogens. The need may also be fulfilled by either exploring antibacterial agents having new mechanism of action or expanding known classes of antibacterial drugs. The paper describes a new chemical entity, compound 21, derived from hitherto little known "floxacin". The choice of the entity was made from a series of synthesized prodrugs and salts of the active chiral benzoquinolizine carboxylic acid, S-(-)-nadifloxacin. The chemistry, physicochemical characteristics, and essential bioprofile of 21 qualifies it for serious consideration as a novel drug entity against hospital infections of multi-drug-resistant Staphylococcus aureus, and its progress up to clinical phase I trials in humans is described.

CiteXplore: 16078842

DOI: 10.1021/jm050035f