Discovery of dual-action phenolic 4-arylidene-isoquinolinones with antioxidant and α-glucosidase inhibition activities.
RSC Med Chem
; 15(2): 519-538, 2024 Feb 21.
Article
em En
| MEDLINE
| ID: mdl-38389895
ABSTRACT
A multicomponent-derived synthesis of arylidene isoquinolinones decorated with phenolic moieties is described. The series demonstrated good DPPH trapping and, in the case of sinapic acid-containing analogs, excellent activity against lipoperoxidation; EPR also demonstrated that one derivative scavenged hydroxyl radicals. In addition, some compounds showed excellent inhibition of α-glucosidase activity and, according to both Lineweaver-Burk plots and molecular docking, they act as non-competitive or mixed inhibitors. In vitro assay also demonstrated that two compounds significantly reduced the plasma glucose levels after sucrose administration. In summary, the studied isoquinolinones become novel compounds with dual action (antioxidant and α-glucosidase inhibition) against diabetes and related metabolic diseases, whose optimization would lead to more potent candidates.
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01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
RSC Med Chem
Ano de publicação:
2024
Tipo de documento:
Article