Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

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 compare...

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Bibliographic Details
Published in:Scientific reports 2022-08, Vol.12 (1), p.14019-14019, Article 14019
Main Authors: Noori, Milad, Davoodi, Ali, Iraji, Aida, Dastyafteh, Navid, Khalili, Minoo, Asadi, Mehdi, Mohammadi Khanaposhtani, Maryam, Mojtabavi, Somayeh, Dianatpour, Mehdi, Faramarzi, Mohammad Ali, Larijani, Bagher, Amanlou, Massoud, Mahdavi, Mohammad
Format: Article
Language:English
Subjects:
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631/154/309
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631/92/607
Acarbose
Design
Diabetes
Diabetes mellitus
Enzymes
Glucose
Humanities and Social Sciences
Hyperglycemia
Imidazole
Metabolism
multidisciplinary
Pharmacy
Research centers
Science
Science (multidisciplinary)
α-Glucosidase
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Summary: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.
ISSN:2045-2322
2045-2322
DOI:10.1038/s41598-022-18455-7