Synthesis and structure–activity relationship studies of phenolic hydroxyl derivatives based on quinoxalinone as aldose reductase inhibitors with antioxidant activity

A novel series of phenolic hydroxyl containing quinoxalinone derivatives were designed and synthesized as potent aldose reductase inhibitors. Compounds 6b and 6f exhibited not only significant ALR2 inhibition and selectivity but also antioxidant properties. Structure-activity relationship and docking studies further confirmed the importance of phenolic hydroxyl for enhancing aldose reductase inhibition and adding antioxidant ability.