1.
Eur J Med Chem
; 46(11): 5524-31, 2011 Nov.
Article
in English
| MEDLINE
| ID: mdl-21944473
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-phenethyl-1H-1,2,3-triazole displayed a minimum inhibitory concentration inferior to 2 µg/mL against Mycobacterium tuberculosis H37Rv.