title: Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents.
abstract: 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.
authors.affiliation: CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, UMR-5068, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France.
authors.forename: Christophe
authors.initials: C
authors.lastname: Menendez
authors.forename: Aurélien
authors.initials: A
authors.lastname: Chollet
authors.forename: Frédéric
authors.initials: F
authors.lastname: Rodriguez
authors.forename: Cyril
authors.initials: C
authors.lastname: Inard
authors.forename: Maria Rosalia
authors.initials: MR
authors.lastname: Pasca
authors.forename: Christian
authors.initials: C
authors.lastname: Lherbet
authors.forename: Michel
authors.initials: M
authors.lastname: Baltas
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000201:enzymology*; D010088:Oxidoreductases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011487:Protein Conformation; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000995:Antitubercular Agents; D001426:Bacterial Proteins; D004791:Enzyme Inhibitors; D014230:Triazoles; D010088:Oxidoreductases; C085257:InhA protein, Mycobacterium