1310064-13-1Relevant articles and documents
Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists
Guay, Daniel,Beaulieu, Christian,Belley, Michel,Crane, Sheldon N.,DeLuca, Jeancarlo,Gareau, Yves,Hamel, Martine,Henault, Martin,Hyjazie, Huda,Kargman, Stacia,Chan, Chi Chung,Xu, Lijing,Gordon, Robert,Li, Lianhai,Mamane, Yael,Morin, Nicolas,Mancini, Joseph,Thérien, Michel,Tranmer, Geoffrey,Truong, Vouy Linh,Wang, Zhaoyin,Black, W. Cameron
, p. 2832 - 2835 (2011/06/24)
A weak antagonist of the pyrimidinergic receptor P2Y14 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 P2Y14 antagonist with good oral bioavailability and provided sufficient exposure in mice to be used as a tool for future in vivo studies.
