Synthesis, biological evaluation and molecular docking study of benzimidazole derivatives as α-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.

Automated summary

This study synthesized benzimidazole derivatives for the treatment of diabetes, which exhibited excellent α-glucosidase inhibitory activity compared to clinically used inhibitors.