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Design, Synthesis, and in Silico Studies of Quinoline-Based-Benzo[D]Imidazole Bearing Different Acetamide Derivatives As Potent Α-Glucosidase Inhibitors Publisher Pubmed



Noori M1 ; Davoodi A2 ; Iraji A3, 4 ; Dastyafteh N1 ; Khalili M1 ; Asadi M2 ; Mohammadi Khanaposhtani M5 ; Mojtabavi S6 ; Dianatpour M3 ; Faramarzi MA6 ; Larijani B1 ; Amanlou M2 ; Mahdavi M1
Authors

Source: Scientific Reports Published:2022


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. © 2022, The Author(s).
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