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.
Eur J Med Chem. 2013 Nov;69:167-73. doi: 10.1016/j.ejmech.2013.06.042. Epub 2013 Jul 8.
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.
合成了两个系列的α-酮三唑和α,β-二酮三唑衍生物，并对其抗结核和细胞毒性活性进行了评价。其中，两个α,β-二酮三唑化合物 6b 和 9b 对结核分枝杆菌和耐多药结核分枝杆菌菌株表现出良好的活性（最小抑菌浓度分别为 7.6 μM 和 6.9 μM），且对结直肠癌细胞 HCT116 和正常成纤维细胞 GM637H 细胞系无细胞毒性（IC₅₀ > 50 μM）。这两个化合物代表了进一步优化的有希望的先导化合物。
