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Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition

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Currently, there is an increasing interest towards -glucosidase inhibition of various diseases including diabetes mellitus type 2, cancer, HIV, and B- and C-type viral hepatitis. Cinnamic acid derivatives have been… Click to show full abstract

Currently, there is an increasing interest towards -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 -glucosidase inhibitors. Therefore, herein, the -glucosidase inhibitory activity of trans-N-cinnamoyl and hydroxycinnamoyl amides was studied in vitro. Results revealed that the tested hydroxycinnamoyl amides (1–16) inhibited a-glucosidase with IC50s ranging between 0.76 and 355.1 μg/ml. Compounds 1, 2, 5, 6, 9, 14, and 15 showed significant inhibition of yeast -glucosidase, being even more potent ones than the used positive inhibitor acarbose (  μg/ml).

Keywords: cinnamoyl hydroxycinnamoyl; hydroxycinnamoyl amides; inhibition; activity; glucosidase inhibition

Journal Title: Journal of Chemistry
Year Published: 2017

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