Article ; Online: Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists.
Journal of medicinal chemistry
2023 Volume 66, Issue 9, Page(s) 6105–6121
Abstract: The free fatty acid receptor 2 (FFA2), also known as GPR43, mediates effects of short-chain fatty acids and has attracted interest as a potential target for treatment of various metabolic and inflammatory diseases. Herein, we report the results from ... ...
| Abstract | The free fatty acid receptor 2 (FFA2), also known as GPR43, mediates effects of short-chain fatty acids and has attracted interest as a potential target for treatment of various metabolic and inflammatory diseases. Herein, we report the results from bioisosteric replacement of the carboxylic acid group of the established FFA2 antagonist CATPB and SAR investigations around these compounds, leading to the discovery of the first high-potency FFA2 antagonists, with the preferred compound TUG-2304 ( |
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| MeSH term(s) | Fatty Acids, Nonesterified ; Propionates ; Receptors, Cell Surface/antagonists & inhibitors ; Receptors, Cell Surface/chemistry ; Receptors, G-Protein-Coupled/metabolism | ||||||||||
| Chemical Substances | Fatty Acids, Nonesterified ; Propionates ; Receptors, Cell Surface ; Receptors, G-Protein-Coupled ; FFA2R protein, human | ||||||||||
| Language | English | ||||||||||
| Publishing date | 2023-05-02 | ||||||||||
| Publishing country | United States | ||||||||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | ||||||||||
| ZDB-ID | 218133-2 | ||||||||||
| ISSN | 1520-4804 ; 0022-2623 | ||||||||||
| ISSN (online) | 1520-4804 | ||||||||||
| ISSN | 0022-2623 | ||||||||||
| DOI | 10.1021/acs.jmedchem.2c01935 | ||||||||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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