1.
Bioorg Med Chem Lett
; 21(10): 2832-5, 2011 May 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21507642
RESUMEN
A weak antagonist of the pyrimidinergic receptor P2Y(14) containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists and represent the first reported non-nucleotide antagonists of this receptor. Compound 18q was identified as a 10 nM P2Y(14) antagonist with good oral bioavailability and provided sufficient exposure in mice to be used as a tool for future in vivo studies.