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Sci Rep ; 12(1): 14019, 2022 08 18.
Artigo em Inglês | MEDLINE | ID: mdl-35982225

RESUMO

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.


Assuntos
Inibidores de Glicosídeo Hidrolases , Quinolinas , Acetamidas , Inibidores de Glicosídeo Hidrolases/química , Imidazóis/farmacologia , Cinética , Simulação de Acoplamento Molecular , Estrutura Molecular , Quinolinas/química , Quinolinas/farmacologia , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismo
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