From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria

…, S Briet, G LeFralliec, C Oliveira, N Desroy…

Index: Gerusz, Vincent; Denis, Alexis; Faivre, Fabien; Bonvin, Yannick; Oxoby, Mayalen; Briet, Sophia; LeFralliec, Geraldine; Oliveira, Chrystelle; Desroy, Nicolas; Raymond, Cedric; Peltier, Laetitia; Moreau, Francois; Escaich, Sonia; Vongsouthi, Vanida; Floquet, Stephanie; Drocourt, Elodie; Walton, Armelle; Prouvensier, Laure; Saccomani, Marc; Durant, Lionel; Genevard, Jean-Marie; Sam-Sambo, Vanessa; Soulama-Mouze, Coralie Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9914 - 9928

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Citation Number: 22

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 ...