期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 69, 期 -, 页码 167-173出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.06.042
关键词
Inhibitor; alpha,beta-Diketotriazole; Tuberculosis; Oxidation; Cytotoxicity
Two series of alpha-ketotriazole and alpha,beta-diketotriazole derivatives were synthesized and evaluated for antitubercular and cytotoxic activities. Among them, two alpha,beta-diketotriazole compounds, 6b and 9b, exhibited good activities (minimum inhibitory concentration = 7.6 mu M and 6.9 mu M, respectively) on Mycobacterium tuberculosis and multi-drug resistant M. tuberculosis strains and presented no cytotoxicity (IC50 > 50 mu M) on colorectal cancer HCT116 and normal fibroblast GM637H cell lines. These two compounds represent promising leads for further optimization. (C) 2013 Elsevier Masson SAS. All rights reserved.
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