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Bioorg Med Chem Lett. 2011 May 15;21(10):2832-5. doi: 10.1016/j.bmcl.2011.03.084. Epub 2011 Mar 30.

Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.

Author information

1
Merck Frosst Center for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8.

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.

PMID:
21507642
DOI:
10.1016/j.bmcl.2011.03.084
[Indexed for MEDLINE]

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