Microwave synthesis, biological evaluation and docking studies of 2-substituted methyl 1-(4-fluorophenyl)-1H-benzimidazole-5-carboxylates
作者： Suhas A. Shintre , Deresh Ramjugernath , Parvesh Singh , Chunderika Mocktar , Neil A. Koorbanally
DOI: 10.1007/S00044-016-1763-Z
关键词:
摘要: A library of 22 novel 2-substituted fluorinated benzimidazoles (5a-v) was synthesized under microwave conditions in yields between 85–96% and tested for their antimicrobial antioxidant activity. Two trioxygenated derivatives 5p 5r had minimum bactericidal concentration values ranging 14.5–115.7 μM (5p) 25.6–74.3 μM (5r) against S. aureus, E. coli, P. aeruginosa K. pneumoniae. The benzimidazole 5e with a CF3 substituent the best antifungal activity at 94.3 µM C. albicans. Compounds also showed good activities 386.6 306.7 µM respectively, comparable to that ascorbic acid. Docking studies 5 h into active site topoisomerase II DNA-gyrase indicated interaction Mn2+ ion enzyme crucial antibacterial
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