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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

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

Volume 10, Issue 3, 2010

Page: [182 - 193] Pages: 12

DOI: 10.2174/138955710791185064

Price: $65

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.

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

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