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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

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 compar...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9386204/
https://www.ncbi.nlm.nih.gov/pubmed/35982225
http://dx.doi.org/10.1038/s41598-022-18455-7
Descripción
Sumario: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.