2. Academic Validation
  3. From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria

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

  • J Med Chem. 2012 Nov 26;55(22):9914-28. doi: 10.1021/jm301113w.
Vincent Gerusz 1,  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
Affiliations

Affiliation

  • 1 Medicinal Chemistry and ‡Biology, Mutabilis, 102 Avenue Gaston Roussel, 93230 Romainville, France. [email protected]
PMID: 23092194 DOI: 10.1021/jm301113w
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.

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