jm050035f_si_001.pdf (89.13 kB)
A Chiral Benzoquinolizine-2-carboxylic Acid Arginine Salt Active against Vancomycin-Resistant Staphylococcus aureus
journal contribution
posted on 2005-08-11, 00:00 authored by 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. KhorakiwalaThere 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.