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Synthesis and Biological Evaluation of 3-Styrylchromone Derivatives as Free Radical Scavengers and α-Glucosidase Inhibitors
2014 Volume 62 Issue 8 Pages 810-815
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2014 Volume 62 Issue 8 Pages 810-815
A series of 3-styrylchromone derivatives (4–20) were synthesized and the structure–activity relationships for α-glucosidase inhibition and antioxidant activities were analyzed. Among the synthesized compounds, compounds 15 and 20, which contain a catechol moiety, showed both potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity (15: EC50=17 µM; 20: EC50=23 µM) and α-glucosidase inhibitory activity (15: IC50=16 µM; 20: IC50=10 µM). Our data suggest that 3-styrylchromone derivatives are novel α-glucosidase inhibitors that have the potential to counteract diet-induced hyperglycemia in diabetes.
