Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on alpha-Glucosidase Inhibition
Abstract
Currently, there is an increasing interest towards alpha-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 of alpha-glucosidase inhibitors.
Therefore, herein, the alpha-glucosidase inhibitory activity of trans-N-cinnamoyl and hydroxycinnamoyl amides was studied in vitro. Results revealed that the tested hydroxycinnamoyl amides (1-16) inhibited alpha-glucosidase with IC(50)s ranging between 0.76 and 355.1 mu g/ml.
Compounds 1, 2, 5, 6, 9, 14, and 15 showed significant inhibition of yeast alpha-glucosidase, being even more potent ones than the used positive inhibitor acarbose (IC50 = 2.50 +/- 0.21 mu g/ml).