Various N-substituted derivatives of 4-O-α-D-glucopyranosylmoranoline have been synthesized, and their inhibitory activities against rabbit sucrase and maltase have been measured, as well as their effects on postprandial hyperglycemia in the sucrose-loaded rat, 4-O-α-D-Glucopyranosylmoranoline was also shown to have potent hypoglycemic activity in starch-loaded dogs.