Design, synthesis and evaluation of l-quebrachitol derivatives against α-glycosidase

Abstract

Two series of L-quebrachitol derivatives have been designed and synthesized in order to search for novel hypoglycemic agents. The α-glycosidase inhibitory activities of these compounds were evaluated, and their structure–activity relationships (SARs) were discussed. Using Acarbose as the positive control, the activities of 16 synthesized compounds against α-glycosidase were evaluated with 4-nitrophenyl-α-D-glucopyranoside as a substrate. The results showed that 16 compounds had significant inhibitory activities against α-glycosidase and 8 compounds (6b, 3b, 3c, 3e, 3h, 3i, 3j, and 3l) out of them had stronger inhibitory activities than Acarbose. Furthermore, 3i has the strongest activity, which is 20 times stronger than that of Acarbose.