| Literature DB >> 15664806 |
Michel Belley1, Michel Gallant, Bruno Roy, Karine Houde, Nicolas Lachance, Marc Labelle, Laird A Trimble, Nathalie Chauret, Chun Li, Nicole Sawyer, Nathalie Tremblay, Sonia Lamontagne, Marie-Claude Carrière, Danielle Denis, Gillian M Greig, Deborah Slipetz, Kathleen M Metters, Robert Gordon, Chi Chung Chan, Robert J Zamboni.
Abstract
A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E(2) receptors evaluated. Many of them are very potent and selective EP(3) antagonists (K(i) 3-10 nM), while compound 9 is a very good and selective EP(2) agonist (K(i) 8 nM). The biological profile of the EP(2) agonist 9 in vivo and the metabolic profile of selected EP(3) antagonists are also reported.Entities:
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Year: 2005 PMID： 15664806 DOI： 10.1016/j.bmcl.2004.11.051
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823