Design, synthesis and antidiabetic study of triazole clubbed indole derivatives as α-glucosidase inhibitors.
Bioorg Chem
; 139: 106750, 2023 10.
Article
en En
| MEDLINE
| ID: mdl-37499530
ABSTRACT
α -Glucosidase is an enzyme present near the brush boundary of the small intestine that is essential in the hydrolysis of carbohydrates to glucose. Because inhibiting this enzyme slows the release of glucose, α-Glucosidase inhibitors are appealing medications for treating diabetes as a carbohydrate-related illness. The present study includes the design, synthesis and antidiabetic potential of novel triazole based indole derivatives as α-glucosidase inhibitor. Among them, the compound R1 was found to be most potent with promising candidate with IC50 value of 10.1 µM and R2 and R3 showed the good inhibitory potency with IC50 values 12.95 µM, 11.35 µM, respectively when compared to the standard drug acarbose having IC50 value of 13.5 µM. In in vivo studies, body weight of the mice was increased when compared to standard drug acarbose, the blood glucose level of the mice was decreased, same as the total cholesterol level, LDL, and triglycerides level decreased in comparison to standard drug. The level HDL was increased as it is a good cholesterol in comparison to standard drug acarbose. Furthermore, these synthesized compounds were docked with α-glucosidase using PDB ID3WY1 which showed that compound R1 having good docking score -6.734 kcal/mol and compound R2, R3 showed docking score -6.14, -6.10 kcal/mol, respectively when compared with standard acarbose having docking score -4.55 kcal/mol. R1 showed the similar interaction with amino acid PHE166, GLU271, comparison with standard drug Acarbose. The synthesized compounds have been confirmed for antidiabetic activity and may be used for further development of potent compounds.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Glicósido Hidrolasas
/
Cardiopatías
Límite:
Animals
Idioma:
En
Revista:
Bioorg Chem
Año:
2023
Tipo del documento:
Article
País de afiliación:
India