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Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents

  作者 Menendez, C; Chollet, A; Rodriguez, F; Inard, C; Pasca, MR; Lherbet, C; Baltas, M  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2012年52-1;  页码  275-283  
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[摘要]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 mu g/ml, respectively. Particularly, compound 12 presenting the best MIC value of all compounds tested (0.6 mu M) is totally inactive against InhA. (C) 2012 Elsevier Masson SAS. All rights reserved.

 
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