Abstract
A series of azines, a class of novel nonsugar α-glucosidase inhibitors, were synthesized with appropriate polyhydroxybenzaldehydes and hydrazine, and their α-glucosidase inhibitory activities were investigated with PNPG as substrate. Compounds 10a, 10b, 10d, 11d, and 11g exhibited good inhibitory activity, with IC50 values less than 1μmolL−1. In particular, compound 10a was the most potent inhibitor of α-glucosidase, with an IC50 value of 0.186μmolL−1. In addition, kinetic studies showed that compounds 10a and 12e exhibited competitive-type inhibition. Herein, we also discuss the mechanisms of inhibition and structure–activity relationships. These results reveal lead compounds and novel alternatives for developing α-glucosidase inhibitors.
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