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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.
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1 Tehran University of Medical Sciences, Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran, Iran (GRID:grid.411705.6) (ISNI:0000 0001 0166 0922)
2 Tehran University of Medical Sciences, Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran, Iran (GRID:grid.411705.6) (ISNI:0000 0001 0166 0922)
3 Shiraz University of Medical Sciences, Stem Cells Technology Research Center, Shiraz, Iran (GRID:grid.412571.4) (ISNI:0000 0000 8819 4698); Shiraz University of Medical Sciences, Central Research Laboratory, Shiraz, Iran (GRID:grid.412571.4) (ISNI:0000 0000 8819 4698)
4 Babol University of Medical Sciences, Cellular and Molecular Biology Research Center, Health Research Institute, Babol, Iran (GRID:grid.411495.c) (ISNI:0000 0004 0421 4102)
5 Tehran University of Medical Sciences, Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran, Iran (GRID:grid.411705.6) (ISNI:0000 0001 0166 0922)
6 Shiraz University of Medical Sciences, Stem Cells Technology Research Center, Shiraz, Iran (GRID:grid.412571.4) (ISNI:0000 0000 8819 4698)