Detalle de: Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists
| Title | Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists |
| Abstract |
We report the first family of 2-acetamidopyridines as potent and selective A 3 adenosine receptor (AR) antagonists. The computer-assisted design was focused on the bioisosteric replacement of the N1 atom by a CH group in a previous series of diarylpyrimidines. Some of the generated 2-acetamidopyridines elicit an antagonistic effect with excellent affinity (K i 3 AR, and exemplifies the benefits of a joint theoretical-experimental approach to identify novel hA 3 AR antagonists through succinct and efficient synthetic methodologies. |
| Apa Reference | Azuaje, J., Jespers, W., Yaziji, V., Mallo, A., Majellaro, M., Caamaño, O., Loza, M. I., Cadavid, M. I., Brea, J., Åqvist, J., Sotelo, E., & Gutiérrez-de-Terán, H. (2017). Effect of Nitrogen Atom Substitution in A3Adenosine Receptor Binding:N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists. Journal of Medicinal Chemistry, 60(17), 7502–7511. 10.1021/acs.jmedchem.7b00860 |
| Doi | 10.1021/acs.jmedchem.7b00860 |
| Publication Date | 21 Aug 2017 |
| Publication Type | Article |
| Researcher | Hugo Gutiérrez de Terán Castañón |
| Ontology | Molecular Interactions/Docking |
| Research Groups | |
| Tools |