| Literature DB >> 15686932 |
Yves Ducharme1, Marc Blouin, Marie-Claude Carrière, Anne Chateauneuf, Bernard Côté, Danielle Denis, Richard Frenette, Gillian Greig, Stacia Kargman, Sonia Lamontagne, Evelyn Martins, François Nantel, Gary O'Neill, Nicole Sawyer, Kathleen M Metters, Richard W Friesen.
Abstract
The synthesis and the EP(1) receptor binding affinity of 2,3-diarylthiophene derivatives are described. The evaluation of the structure-activity relationship (SAR) in this series led to the identification of compounds 4, 7, and 12a, which exhibit high affinity for the human EP(1) receptor and a selectivity greater than 100-fold against the EP(2), EP(3), EP(4), DP, FP, and IP receptors and greater than 25-fold versus the TP receptor. These three antagonists present good pharmacokinetics in rats and significant differences in the way they are distributed in the brain.Entities:
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Year: 2005 PMID： 15686932 DOI： 10.1016/j.bmcl.2004.12.005
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823