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Synthesis and antitubercular screening of imidazole derivatives.

机译:咪唑衍生物的合成和抗结核筛选。

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摘要

A series of imidazole based compounds were synthesized by reacting simple imidazoles with alkyl halides or alkyl halocarboxylate in presence of tetrabutylammonium bromide (TBAB). The compounds bearing carbethoxy group undergo amidation with different amines in the presence of DBU to give respective carboxamides. The synthesized compounds were screened against Mycobacterium tuberculosis where compound 17 exhibited very good in vitro antitubercular activity and may serve as a lead for further optimization.
机译:通过使简单的咪唑与烷基卤化物或烷基卤代羧酸盐在四丁基溴化铵(TBAB)存在下反应,合成了一系列基于咪唑的化合物。在DBU存在下,带有甲乙氧基的化合物与不同的胺酰胺化,得到各自的羧酰胺。对合成的化合物进行了针对结核分枝杆菌的筛选,其中化合物17表现出非常好的体外抗结核活性,并可作为进一步优化的线索。

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