Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

In this study, 18 novel quinoline-based-benzo[d]imidazole derivatives were synthesized and screened for their alpha-glucosidase inhibitory potential. All compounds in the series except 9q showed a significant alpha-glucosidase inhibition with IC50 values in the range of 3.2 +/- 0.3-185.0 +/- 0.3 mu M, as compared to the standard drug acarbose (IC50 = 750.0 +/- 5.0 mu M). A kinetic study indicated that compound 9d as the most potent derivative against alpha-glucosidase was a competitive type inhibitor. Furthermore, the molecular docking study revealed the effective binding interactions of 9d with the active site of the alpha-glucosidase enzyme. The results indicate that the designed compounds have the potential to be further studied as new anti-diabetic agents.

Automated summary

In this study, 18 novel quinoline-based-benzo[d]imidazole derivatives were synthesized and screened for their alpha-glucosidase inhibitory potential. Except for 9q, all compounds in the series exhibited significant α-glucosidase inhibition, with compound 9d showing the most potent competitive inhibition. Molecular docking study indicated effective binding interactions between the designed compounds, including 9d, and the active site of the alpha-glucosidase enzyme.