107572-70-3Relevant articles and documents
α-Glucosidase inhibition of 6-hydroxyflavones. Part 3: Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as α-glucosidase inhibitors
Gao, Hong,Kawabata, Jun
, p. 1661 - 1671 (2007/10/03)
The SAR studies suggested that the C-ring of baicalein (1) was not necessary for the activity, and validated the importance of 2,3,4- trihydroxybenzoyl structure of 1. Thus, a series of 2,3,4-trihydroxybenzoyl- containing flavonoid analogs were investigat
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors
Costantino, Luca,Rastelli, Giulio,Gamberini, Maria Cristina,Vinson, Joe A.,Bose, Pratima,Iannone, Anna,Staffieri, Mariagrazia,Antolini, Luciano,Del Corso, Antonella,Mura, Umberto,Albasini, Albano
, p. 1881 - 1893 (2007/10/03)
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 pK(a) 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.
