2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Basic Information
ID: ALA1144328
Journal: Bioorg Med Chem Lett
Title: 2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Authors: Ducharme Y, Blouin M, Carrière MC, Chateauneuf A, Côté B, Denis D, Frenette R, Greig G, Kargman S, Lamontagne S, Martins E, Nantel F, O'Neill G, Sawyer N, Metters KM, Friesen RW.
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.
CiteXplore: 15686932
DOI: 10.1016/j.bmcl.2004.12.005
Patent ID: ┄