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

Journal of Medicinal Chemistry
V GeruszC 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.

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Citations

Sep 15, 2015·Organic Letters·Nicholas A IsleyBruce H Lipshutz
Jul 12, 2016·Expert Opinion on Therapeutic Patents·Jan Zitko, Martin Doležal
Jan 28, 2017·Future Medicinal Chemistry·Thales KronenbergerVinicius Gonçalves Maltarollo
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Nov 19, 2014·Antimicrobial Agents and Chemotherapy·Joshua B ParsonsCharles O Rock
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Jun 2, 2020·Chemical & Pharmaceutical Bulletin·Hiromichi Egami
Feb 5, 2015·The Journal of Biological Chemistry·Jiangwei Yao, Charles O Rock
Jan 28, 2017·Future Medicinal Chemistry·Thales KronenbergerVinicius Gonçalves Maltarollo
Jan 9, 2017·Journal of Molecular Modeling·Xuyun YangYue Liu
Sep 22, 2020·ACS Omega·Robel DemissieLeslie W-M Fung

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