| Literature DB >> 23092194 |
Vincent Gerusz1, Alexis Denis, Fabien Faivre, Yannick Bonvin, Mayalen Oxoby, Sophia Briet, Géraldine LeFralliec, Chrystelle Oliveira, Nicolas Desroy, Cédric Raymond, Laëtitia Peltier, François Moreau, Sonia Escaich, Vanida Vongsouthi, Stéphanie Floquet, Elodie Drocourt, Armelle Walton, Laure Prouvensier, Marc Saccomani, Lionel Durant, Jean-Marie Genevard, Vanessa Sam-Sambo, Coralie Soulama-Mouze.
Abstract
In this paper, we present some elements of our optimization program to decouple triclosan's specific FabI effect from its nonspecific cytotoxic component. The implementation of this strategy delivered highly specific, potent, and nonbiocidal new FabI inhibitors. We also disclose some preclinical data of one of their representatives, 83, a novel antibacterial compound active against resistant staphylococci and some clinically relevant Gram negative bacteria that is currently undergoing clinical trials.Entities:
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Year: 2012 PMID： 23092194 DOI： 10.1021/jm301113w
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446