title: Synthesis and evaluation of α-ketotriazoles and α,β-diketotriazoles as inhibitors of Mycobacterium tuberculosis.
abstract: Two series of α-ketotriazole and α,β-diketotriazole derivatives were synthesized and evaluated for antitubercular and cytotoxic activities. Among them, two α,β-diketotriazole compounds, 6b and 9b, exhibited good activities (minimum inhibitory concentration = 7.6 μM and 6.9 μM, respectively) on Mycobacterium tuberculosis and multi-drug resistant M. tuberculosis strains and presented no cytotoxicity (IC₅₀ > 50 μM) on colorectal cancer HCT116 and normal fibroblast GM637H cell lines. These two compounds represent promising leads for further optimization.
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; Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 route de Narbonne, F-31062 Toulouse cedex 9, France.
authors.forename: Christophe
authors.initials: C
authors.lastname: Menendez
authors.forename: Frédéric
authors.initials: F
authors.lastname: Rodriguez
authors.forename: Ana Luisa de Jesus Lopes
authors.initials: AL
authors.lastname: Ribeiro
authors.forename: Francesca
authors.initials: F
authors.lastname: Zara
authors.forename: Céline
authors.initials: C
authors.lastname: Frongia
authors.forename: Valérie
authors.initials: V
authors.lastname: Lobjois
authors.forename: Nathalie
authors.initials: N
authors.lastname: Saffon
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: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D045325:HCT116 Cells; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D007659:Ketones; D014230:Triazoles
keywords: Cytotoxicity; Inhibitor; Oxidation; Tuberculosis; α,β-Diketotriazole