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

Noel J. De Souza, Shrikant V. Gupte, Prasad K. Deshpande, Vijaya N. Desai, Satish B. Bhawsar, Ravindra D. Yeole, Milind C. Shukla, Jacob Strahilevitz, David C. Hooper, Bülent Bozdogan, Peter C. Appelbaum, Michael R. Jacobs, Nitin Shetty, Mahesh V. Patel*, Rasendrakumar Jha, Habil F. Khorakiwala

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

46 Scopus citations

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.

Original languageAmerican English
Pages (from-to)5232-5242
Number of pages11
JournalJournal of Medicinal Chemistry
Volume48
Issue number16
DOIs
StatePublished - 11 Aug 2005
Externally publishedYes

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