Synthesis, biological evaluation and molecular docking study of benzimidazole derivatives as alpha-glucosidase inhibitors and anti-diabetes candidates

Voglibose and acarbose are distinguished alpha-glucosidase inhibitors used for controlling diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subse-quently, there is still a need to develop safer therapy. Despite a broad spectrum of the biological im-portance of benzimidazole, it is occasionally evaluated for alpha-glucosidase activity. The current study deals with the synthesis and biological screening of benzimidazole derivatives (1-17) for their alpha-glucosidase inhibitory activity. All derivatives showed an excellent to good inhibitory potential with IC50values 3.40 +/- 0.10 to 36.90 +/- 0.90 mu M as compared to standard drug acarbose (IC50 = 38.60 +/- 0.20 mu M). Among the series, derivative 17 was the most potent one with IC50 value 3.40 +/- 0.10 mu M and all other derivatives +/- 0.60, 28.60 +/- 0.60, 28.80 +/- 0.60, 32.40 +/- 0.70 and36.50 +/- 0.90 mu M respectively which were many fold better as compare to standard drug. The structure-activity relationship was established and binding interactions were confirmed through molecular docking studies. (c) 2022 Elsevier B.V. All rights reserved.