- From triclosan toward the clinic: Discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria
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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.
- Gerusz, Vincent,Denis, Alexis,Faivre, Fabien,Bonvin, Yannick,Oxoby, Mayalen,Briet, Sophia,LeFralliec, Géraldine,Oliveira, Chrystelle,Desroy, Nicolas,Raymond, Cédric,Peltier, La?titia,Moreau, Fran?ois,Escaich, Sonia,Vongsouthi, Vanida,Floquet, Stéphanie,Drocourt, Elodie,Walton, Armelle,Prouvensier, Laure,Saccomani, Marc,Durant, Lionel,Genevard, Jean-Marie,Sam-Sambo, Vanessa,Soulama-Mouze, Coralie
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supporting information
p. 9914 - 9928
(2013/01/16)
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- Hydroxyphenyl derivatives and biological applications thereof
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The invention relates to hydroxyphenyl derivatives of formula (I) and the pharmaceutically acceptable salts, the organic and mineral salts, the racemic and each non racemic derivatives, the cis (Z) and Lrans (E) isomers the tautomers. Application particularly as anti-bacterial and/or anti-parasite agents.
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Page/Page column 39
(2008/06/13)
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