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

Currently, there is an increasing interest towards α-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 α-glucosidase inhibitors. Therefo...

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Published in:Journal of chemistry 2017-01, Vol.2017 (2017), p.1-5
Main Authors: Milkova, Tsenka S., Štícha, Martin, Ivanova, G., Stoykova, Boyka M., Petrova, Petranka P., Chochkova, Maya G., Dibó, Gábor
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Language:English
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cited_by cdi_FETCH-LOGICAL-c360t-8208e48fe7f480ba326acac2cde799bc20f8dd2a38232d9d9a3949e560fcf5303
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container_issue 2017
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container_title Journal of chemistry
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creator Milkova, Tsenka S.
Štícha, Martin
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description Currently, there is an increasing interest towards α-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 α-glucosidase inhibitors. Therefore, herein, the α-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 α-glucosidase, being even more potent ones than the used positive inhibitor acarbose (IC50=2.50±0.21 μg/ml).
doi_str_mv 10.1155/2017/6080129
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title Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition
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