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Letters in Organic Chemistry

Editor-in-Chief

ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Synthesis of an Indoloquinoxaline Derivative as Potential Inhibitor of InhA enzyme of Mycobacterium tuberculosis

Author(s): Asmae Zanzoul, Aurélien Chollet, Estefania Piedra-Arroni, Jean-Luc Stigliani, Vania Bernardes-Génisson, El Mokhtar Essassi and Geneviève Pratviel

Volume 12 , Issue 10 , 2015

Page: [727 - 733] Pages: 7

DOI: 10.2174/1570178612666150924000909

Price: $65

Abstract

Seven heterocyclic compounds derived from isatin have been synthesized. Isatin was N-substituted with four aromatic/aliphatic and benzylic moieties (1a-d). Compounds 1a-c were condensed with o-phenylenediamine to afford indoloquinoxaline derivatives (2a-c). Products were tested as inhibitors of InhA enzyme of M. tuberculosis. Compound 6-(diethylaminoethyl)indoloquinoxaline (2a) inhibited 38% of InhA activity at 50 µM. The possible modes of interaction of 2a with InhA were explored by molecular docking. Docking experiments afford keys to improve compound 2a for the design of new potential active drugs against tuberculosis.

Keywords: Heterocyclic compounds, InhA inhibition, modeling, tuberculosis.


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