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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| Format: | Article |
| Language: | English |
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Wiley
2017-01-01
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| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2017/6080129 |
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| author | Maya G. Chochkova Petranka P. Petrova Boyka M. Stoykova Galya I. Ivanova Martin Štícha Gábor Dibó Tsenka S. Milkova |
| author_facet | Maya G. Chochkova Petranka P. Petrova Boyka M. Stoykova Galya I. Ivanova Martin Štícha Gábor Dibó Tsenka S. Milkova |
| author_sort | Maya G. Chochkova |
| collection | DOAJ |
| 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). |
| format | Article |
| id | doaj-art-e8baae40d24b4c6f8454d037a4f07707 |
| institution | DOAJ |
| issn | 2090-9063 2090-9071 |
| language | English |
| publishDate | 2017-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-e8baae40d24b4c6f8454d037a4f077072025-08-20T03:21:09ZengWileyJournal of Chemistry2090-90632090-90712017-01-01201710.1155/2017/60801296080129Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase InhibitionMaya G. Chochkova0Petranka P. Petrova1Boyka M. Stoykova2Galya I. Ivanova3Martin Štícha4Gábor Dibó5Tsenka S. Milkova6Faculty of Mathematics and Natural Sciences, South-West University “Neofit Rilski”, 66 Ivan Mihailov Str., 2700 Blagoevgrad, BulgariaFaculty of Mathematics and Natural Sciences, South-West University “Neofit Rilski”, 66 Ivan Mihailov Str., 2700 Blagoevgrad, BulgariaFaculty of Mathematics and Natural Sciences, South-West University “Neofit Rilski”, 66 Ivan Mihailov Str., 2700 Blagoevgrad, BulgariaREQUIMTE-UCIBIO, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre s/n, 4169-007 Porto, PortugalFaculty of Science, Section of Chemistry, Charles University, Hlavova 2030/8, 12843 Prague 2, Czech RepublicFaculty of Education, Department of Chemistry, Janos Selye University, Bratislavská Cesta 3322, 94501 Komárno, SlovakiaFaculty of Mathematics and Natural Sciences, South-West University “Neofit Rilski”, 66 Ivan Mihailov Str., 2700 Blagoevgrad, BulgariaCurrently, 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).http://dx.doi.org/10.1155/2017/6080129 |
| spellingShingle | Maya G. Chochkova Petranka P. Petrova Boyka M. Stoykova Galya I. Ivanova Martin Štícha Gábor Dibó Tsenka S. Milkova Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition Journal of Chemistry |
| title | Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition |
| title_full | Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition |
| title_fullStr | Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition |
| title_full_unstemmed | Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition |
| title_short | Structure-Activity Relationships of N-Cinnamoyl and Hydroxycinnamoyl Amides on α-Glucosidase Inhibition |
| title_sort | structure activity relationships of n cinnamoyl and hydroxycinnamoyl amides on α glucosidase inhibition |
| url | http://dx.doi.org/10.1155/2017/6080129 |
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