Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.

Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.
Eur J Med Chem. 2019 Dec 24;188:112010
Authors: Sirim MM, Krishna VS, Sriram D, Unsal Tan O
Abstract
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.
PMID: 31893548 [PubMed - as supplied by publisher]

Source: European Journal of Medicinal Chemistry - December 23, 2019 Category: Chemistry Authors: Sirim MM, Krishna VS, Sriram D, Unsal Tan O Tags: Eur J Med Chem Source Type: research