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.
Eur J Med Chem. 2012 Jun;52:275-83. doi: 10.1016/j.ejmech.2012.03.029. Epub 2012 Mar 23.
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.
已经制备了一系列三唑类化合物，并将其评估为 InhA 抑制剂和结核分枝杆菌 H(37)R(v)抑制剂。这些新化合物中的几种对 InhA 具有良好的活性，特别是化合物 17 和 18，对其进行了分子对接。关于它们对结核分枝杆菌 H(37)R(V)菌株的活性，其中两种化合物 3 和 12 被发现是良好的抑制剂，MIC 值分别为 0.50 和 0.25μg/mL。特别是，在所测试的所有化合物中 MIC 值最低的化合物 12（0.6μM）对 InhA 完全没有活性。
