Detalle de: Discovery of 3,4-Dihydropyrimidin-2(1 H )-ones As a Novel Class of Potent and Selective A 2B Adenosine Receptor Antagonists
| Title | Discovery of 3,4-Dihydropyrimidin-2(1 H )-ones As a Novel Class of Potent and Selective A 2B Adenosine Receptor Antagonists |
| Abstract |
We describe the discovery and optimization of 3,4-dihydropyrimidin-2(1H)-ones as a novel family of (nonxanthine) A2B receptor antagonists that exhibit an unusually high selectivity profile. The Biginelli-based hit optimization process enabled a thoughtful exploration of the structure-activity and structure-selectivity relationships for this chemotype, enabling the identification of ligands that combine structural simplicity with excellent hA2B AdoR affinity and remarkable selectivity profiles. |
| Apa Reference | Crespo, A., El Maatougui, A., Biagini, P., Azuaje, J., Coelho, A., Brea, J., Loza, M.I., Cadavid, M.I., García-Mera, X., Gutiérrez-de-Terán, H. & Sotelo, E. (2013). Discovery of 3,4-Dihydropyrimidin-2(1 H )-ones As a Novel Class of Potent and Selective A 2B Adenosine Receptor Antagonists. ACS Medicinal Chemistry Letters, 4(11), 1031-1036. 10.1021/ml400185v |
| Doi | 10.1021/ml400185v |
| Publication Date | 4 Oct 2013 |
| Publication Type | Article |
| Researcher | Hugo Gutiérrez de Terán Castañón |
| Ontology | Structure-function relationship, Molecular Interactions/Docking |
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