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

• Published in: European journal of medicinal chemistry 2020-02, Vol.188, p.112010-112010, Article 112010
• Main Authors: Sirim, Mustafa Mert, Krishna, Vagolu Siva, Sriram, Dharmarajan, Unsal Tan, Oya
• Format: Article
• Language: English
• Subjects: Acrylonitrile; Antimycobacterial activity; Benzimidazole; Nutrient starvation test; Propanenitrile
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2019.112010

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. [Display omitted] •Novel benzimidazole-acrylonitrile hybrid derivatives were designed and synthesized.•The compounds were evaluated against Mycobacterium tuberculosis H37Rv (Mtb).•3a, 3b and 3g showed remarkable activity (MtbMIC = 0.78–6.25 μg/mL).•3b is also effective against dormant forms of Mtb.