Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors
Milad Noori, Ali Davoodi, Aida Iraji, Navid Dastyafteh, Minoo Khalili, Mehdi Asadi, Maryam Mohammadi‐Khanaposhtani, Somayeh Mojtabavi, Mehdi Dianatpour, Mohammad Ali Faramarzi, Bagher Larijani, Massoud Amanlou, Mohammad Mahdavi
Abstract
Abstract In this study, 18 novel quinoline-based-benzo[d]imidazole derivatives were synthesized and screened for their α-glucosidase inhibitory potential. All compounds in the series except 9q showed a significant α-glucosidase inhibition with IC 50 values in the range of 3.2 ± 0.3–185.0 ± 0.3 µM, as compared to the standard drug acarbose (IC 50 = 750.0 ± 5.0 µM). A kinetic study indicated that compound 9d as the most potent derivative against α-glucosidase was a competitive type inhibitor. Furthermore, the molecular docking study revealed the effective binding interactions of 9d with the active site of the α-glucosidase enzyme. The results indicate that the designed compounds have the potential to be further studied as new anti-diabetic agents.