Structure-Activity Relationships ofN-Cinnamoyl and Hydroxycinnamoyl Amides onα-Glucosidase Inhibition

Abstract

Currently, there is an increasing interest towardsα-glucosidase inhibition of various diseases including diabetes mellitus type 2, cancer, HIV, and B- and C-type viral hepatitis. Cinnamic acid derivatives have been shown to be potentially valuable as a new group ofα-glucosidase inhibitors. Therefore, herein, theα-glucosidase inhibitory activity oftrans-N-cinnamoyl and hydroxycinnamoyl amides was studied in vitro. Results revealed that the tested hydroxycinnamoyl amides (1–16) inhibiteda-glucosidase with IC50s ranging between 0.76 and 355.1 μg/ml. Compounds1,2,5,6,9,14, and15showed significant inhibition of yeastα-glucosidase, being even more potent ones than the used positive inhibitor acarbose (IC50=2.50±0.21 μg/ml).