| Literature DB >> 21507642 |
Daniel Guay1, Christian Beaulieu, Michel Belley, Sheldon N Crane, Jeancarlo DeLuca, Yves Gareau, Martine Hamel, Martin Henault, Huda Hyjazie, Stacia Kargman, Chi Chung Chan, Lijing Xu, Robert Gordon, Lianhai Li, Yael Mamane, Nicolas Morin, Joseph Mancini, Michel Thérien, Geoffrey Tranmer, Vouy Linh Truong, Zhaoyin Wang, W Cameron Black.
Abstract
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.Entities:
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Year: 2011 PMID： 21507642 DOI： 10.1016/j.bmcl.2011.03.084
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823