Synthetic piperidine-substituted chalcones as potential hits for α-amylase inhibitory and antioxidant activities.
Future Med Chem
; 15(6): 497-515, 2023 03.
Article
en En
| MEDLINE
| ID: mdl-37092302
ABSTRACT
Background:
In medicinal chemistry, searching for new therapeutic entities to treat diabetes mellitus is of great concern. The piperidinyl-substituted chalcone scaffold has piqued our interest as a potential antidiabetic agent.Methods:
A variety of piperidinyl-substituted chalcones 2-28 were synthesized and tested for α-amylase inhibitory and 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical-scavenging activities.Results:
Compared with the standard acarbose, all compounds inhibited α-amylase, with IC50 values of 9.86-35.98 µM. Docking studies revealed an important binding interaction with the enzyme's catalytic site. The compounds also demonstrated promising radical-scavenging potential against 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radicals.Conclusion:
This study has identified potential lead candidates for further advanced research searching for antidiabetic agents.Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Chalconas
/
Antioxidantes
Idioma:
En
Revista:
Future Med Chem
Año:
2023
Tipo del documento:
Article
País de afiliación:
Pakistán