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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.


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.

SUBMITTER: Noori M 

PROVIDER: S-EPMC9386204 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature

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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.

Noori Milad M   Davoodi Ali A   Iraji Aida A   Dastyafteh Navid N   Khalili Minoo M   Asadi Mehdi M   Mohammadi Khanaposhtani Maryam M   Mojtabavi Somayeh S   Dianatpour Mehdi M   Faramarzi Mohammad Ali MA   Larijani Bagher B   Amanlou Massoud M   Mahdavi Mohammad M  

Scientific reports 20220818 1


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<sub>50</sub> values in the range of 3.2 ± 0.3-185.0 ± 0.3 µM, as compared to the standard drug acarbose (IC<sub>50</sub> = 750.0 ± 5.0 µM). A kinetic study indicated that compound 9d as the most potent derivative against α-glucosidase was a competitive type inhi  ...[more]

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