Recent Progress in the Identification and Development of InhA Direct Inhibitors of Mycobacterium tuberculosis

Title: Recent Progress in the Identification and Development of InhA Direct Inhibitors of Mycobacterium tuberculosis

Volume: 10 Issue: 3

Author(s): X.Y. Lu, Q.D. You and Y.D. Chen

Affiliation:

Keywords: InhA, Anti-tubercular agents, Isoniazid, KatG, INH-NAD adduct, Indirect inhibitors, Direct inhibitors, Drug design

Abstract: The InhA-related enoyl-ACP reductase, an enzyme involved in fatty acid synthesis, is one of the best validated targets for the development of anti-tubercular agents. However, the majority of isoniazid (INH)-resistant clinical strains are observed mainly due to the emergence of KatG mutants that do not form an INH-NAD adduct. Thus compounds that directly inhibit InhA avoiding activation by KatG would be promising candidates for combating MDR-TB. Herein, some predominant examples of InhA direct inhibitors recently developed are reviewed and special attention is paid to 3Dstructures of InhA in drug design process.

Cite this article as:

Lu X.Y., You Q.D. and Chen Y.D., Recent Progress in the Identification and Development of InhA Direct Inhibitors of Mycobacterium tuberculosis, Mini-Reviews in Medicinal Chemistry 2010; 10 (3) . https://dx.doi.org/10.2174/138955710791185064