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

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

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 10 , Issue 3 , 2010

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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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Article Details

VOLUME: 10
ISSUE: 3
Year: 2010
Page: [182 - 193]
Pages: 12
DOI: 10.2174/138955710791185064
Price: $58

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PDF: 12