Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors
oleh: 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
| Format: | Article |
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| Diterbitkan: | Nature Portfolio 2022-08-01 |
Deskripsi
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 IC50 values in the range of 3.2 ± 0.3–185.0 ± 0.3 µM, as compared to the standard drug acarbose (IC50 = 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.