Bioorganic and Medicinal Chemistry Letters p. 1155 - 1160 (2005)
Update date:2022-07-30
Topics:
Ducharme, Yves
Blouin, Marc
Carriere, Marie-Claude
Chateauneuf, Anne
Cote, Bernard
Denis, Danielle
Frenette, Richard
Greig, Gillian
Kargman, Stacia
Lamontagne, Sonia
Martins, Evelyn
Nantel, Francois
O'Neill, Gary
Sawyer, Nicole
Metters, Kathleen M.
Friesen, Richard W.
The synthesis and the EP1 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 EP2, EP3, EP4, 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.
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