1-Benzopyran-4-one Antioxidants as Aldose Reductase Inhibitors
Year: 1999
Type: article
Abstract: 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.
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm980441h
Language: English
Topic: Aldose Reductase and Taurine
Subfield: Cell Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2020108404