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

Sirim M. M., Krishna V. S., Sriram D., Tan O.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.188, 2020 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 188
  • Basım Tarihi: 2020
  • Doi Numarası: 10.1016/j.ejmech.2019.112010
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, CAB Abstracts, Chimica, EMBASE, MEDLINE, Veterinary Science Database
  • Hacettepe Üniversitesi Adresli: Evet

Özet

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 mu g/mL against M. tuberculosis. This is a quite good activity compared with ethambutol (MIC = 1.56 mu g/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. (C) 2019 Elsevier Masson SAS. All rights reserved.