Synthesis and evaluation of four hederagenin glycosides as α-glucosidase inhibitor

摘要

The four hederagenin glycosides 1-4 were efficiently synthesized through one-pot sequential glycosylations with glycose 1-(trichloroacetimidate)s as donors, resulting in a significantly simplified synthetic procedure without isolation of glycosylation intermediates. The activity of the synthetic hederagenin glycosides 1-4 against α-glucosidase type IV was evaluated; hederagenin glycoside 4 containing an α-L-rhamnopyranosyl unit showed the best activity with an IC_(50) value of 47.9 μM.