1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
J Med Chem
; 42(11): 1881-93, 1999 Jun 03.
Article
en En
| MEDLINE
| ID: mdl-10354396
Starting from the inhibitory activity of the flavonoid Quercetin, a series of 4H-1-benzopyran-4-one derivatives was synthesized and tested for inhibition of aldose reductase, an enzyme involved in the appearance of diabetic complications. Some of the compounds obtained display inhibitory activity similar to that of Sorbinil but are more selective than Quercetin and Sorbinil with respect to the closely related enzyme, aldehyde reductase, and also possess antioxidant activity. Remarkably, these compounds possess higher pKa values than carboxylic acids, a characteristic which could make the pharmacokinetics of these compounds very interesting. Molecular modeling investigations on the structures of inhibitors bound at the active site of aldose reductase were performed in order to suggest how these new inhibitors might bind to the enzyme and also to interpret structure-activity relationships.
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Banco de datos:
MEDLINE
Asunto principal:
Benzopiranos
/
Aldehído Reductasa
/
Inhibidores Enzimáticos
/
Antioxidantes
Tipo de estudio:
Prognostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
1999
Tipo del documento:
Article
País de afiliación:
Italia