Synthesis and biological activities of triazole derivatives as inhibitors of InhA and antituberculosis agents

C Menendez, S Gau, C Lherbet, F Rodriguez…

Index: Menendez, Christophe; Gau, Sylvain; Lherbet, Christian; Rodriguez, Frederic; Inard, Cyril; Pasca, Maria Rosalia; Baltas, Michel European Journal of Medicinal Chemistry, 2011 , vol. 46, # 11 p. 5524 - 5531

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Citation Number: 42

Abstract

InhA, the enoyl reductase from the mycobacterial type II fatty acid biosynthesis pathway, is a target for the development of novel drugs against tuberculosis. We exploited copper- catalyzed [3+ 2] cycloaddition between alkynes and different azides to afford 1, 4- disubstituted triazole or α-ketotriazole derivatives. Several compounds bearing a lipophilic chain mimicking the substrate were able to inhibit InhA. Among them, 1-dodecyl-4- ...