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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

Authors :
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
Source :
Scientific reports. 12(1)
Publication Year :
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.

Details

ISSN :
20452322
Volume :
12
Issue :
1
Database :
OpenAIRE
Journal :
Scientific reports
Accession number :
edsair.doi.dedup.....12508fd8e00b7ed6856bc0a8adb3c9f7