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Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2019-12-24 , DOI: 10.1016/j.ejmech.2019.112010
Mustafa Mert Sirim 1 , Vagolu Siva Krishna 2 , Dharmarajan Sriram 2 , Oya Unsal Tan 1
Affiliation  

This paper reports the synthesis and evaluation of some benzimidazole-acrylonitrile hybrid derivatives for their in vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv. Among the derivatives studied, 3b was found to be the most active compound with MIC of 0.78 μg/mL against M. tuberculosis. This is a quite good activity compared with ethambutol (MIC = 1.56 μg/mL). Moreover, 3b showed 2.8 log fold reduction in bacterial count of dormant forms of mycobacterium which is more potent than first line drugs isoniazid, ciprofloxacin, rifampicin and moxifloxacin. Having activities against both active and dormant forms of M. tuberculosis,3b may be a useful candidate for the development of new drugs to treat tuberculosis.

中文翻译:

新型苯并咪唑-丙烯腈杂化物及其衍生物:设计,合成和抗分枝杆菌活性。

本文报道了一些苯并咪唑-丙烯腈杂化衍生物的合成及其对结核分枝杆菌H37Rv的体外抗分枝杆菌活性的评价。在研究的衍生物中,发现3b是最有效的化合物,对结核分枝杆菌的MIC为0.78μg/ mL。与乙胺丁醇(MIC = 1.56μg/ mL)相比,这是一个相当不错的活性。而且,3b显示休眠形式的分枝杆菌的细菌计数减少2.8 log倍,比一线药物异烟肼,环丙沙星,利福平和莫西沙星更有效。对活性和休眠形式的结核分枝杆菌3b都具有活性,可能是开发治疗结核病的新药的有用候选人。
更新日期:2019-12-25
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