Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents.
Menendez C, Chollet A, Rodriguez F, Inard C, Pasca MR, Lherbet C, Baltas M.
A series of triazoles have been prepared and evaluated as inhibitors of InhA as well as inhibitors of Mycobacterium tuberculosis H(37)R(v). Several of these new compounds possess a good activity against InhA, particularly compounds 17 and 18 for which molecular docking has been performed. Concerning their activities against M. tuberculosis H(37)R(V) strain, two of them, 3 and 12, were found to be good inhibitors with MIC values of 0.50 and 0.25 μg/mL, respectively. Particularly, compound 12 presenting the best MIC value of all compounds tested (0.6 μM) is totally inactive against InhA.