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Joel S. Freundlich, Feng Wang, Catherine Vilchèze, Gulcin Gulten, Robert Langley, Guy A. Schiehser, David P. Jacobus, William R. Jacobs Jr. and James C. Sacchettini Triclosan Derivatives: Towards Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis ChemMedChem 4

Version of Record online: 7 JAN 2009 | DOI: 10.1002/cmdc.200800261

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Overcoming resistance: Isoniazid (INH) is a frontline antitubercular drug that inhibits the enoyl acyl carrier protein reductase InhA. Novel inhibitors of InhA that are not cross-resistant to INH represent a significant goal in antitubercular chemotherapy. The design, synthesis, and biological activity of a series of triclosan-based inhibitors is reported, including their promising efficacy against INH-resistant strains of M. tuberculosis.

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