A series of different substituted isatin derivatives were designed and synthesized about 15-40% overall yields. Three compounds 3a, 3b and 3c have not been reported before. Their structures were characterized by 1H and 13C NMR. All the synthesized derivatives were subjected to evaluate theα-glycosidase inhibitory activity. The results indicated that compounds 3a, 3band 3d exhibited α-glycosidase enzyme inhibition activity.