咪唑衍生物的合成与抗结核筛选
Synthesis and antitubercular screening of imidazole derivatives.
作者信息
Pandey Jyoti, Tiwari Vinod K, Verma Shyam S, Chaturvedi Vinita, Bhatnagar S, Sinha S, Gaikwad A N, Tripathi Rama P
机构信息
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India.
出版信息
Eur J Med Chem. 2009 Aug;44(8):3350-5. doi: 10.1016/j.ejmech.2009.02.013. Epub 2009 Feb 20.
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.
通过在四丁基溴化铵（TBAB）存在下使简单咪唑与卤代烃或卤代羧酸烷基酯反应，合成了一系列基于咪唑的化合物。带有乙氧羰基的化合物在DBU存在下与不同的胺进行酰胺化反应，得到相应的羧酰胺。对合成的化合物针对结核分枝杆菌进行了筛选，其中化合物17表现出非常好的体外抗结核活性，可作为进一步优化的先导化合物。
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