| Literature DB >> 16078842 |
Noel J de Souza1, 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.
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.Entities:
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Year: 2005 PMID： 16078842 DOI： 10.1021/jm050035f
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446