Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science - Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad, 500 078, Andhra Pradesh, India.
Eur J Med Chem. 2020 Feb 15;188:112010. doi: 10.1016/j.ejmech.2019.112010. Epub 2019 Dec 24.
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.
本文报道了一些苯并咪唑-丙烯腈杂合衍生物的合成与评价，以评估它们对结核分枝杆菌 H37Rv 的体外抗分枝杆菌活性。在所研究的衍生物中，发现 3b 对 M. tuberculosis 的 MIC 为 0.78μg/mL，是最具活性的化合物。与乙胺丁醇（MIC=1.56μg/mL）相比，这是一个相当好的活性。此外，3b 对休眠形式的分枝杆菌的细菌计数减少了 2.8 对数级，比一线药物异烟肼、环丙沙星、利福平和莫西沙星更有效。3b 对结核分枝杆菌的活性和休眠形式均具有活性，可能是开发治疗结核病的新药的有用候选药物。
