2,3-Diarylthiophenes as selective EP1 receptor antagonists |
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| Authors: | Ducharme Yves Blouin Marc Carrière Marie-Claude Chateauneuf Anne Côté Bernard Denis Danielle Frenette Richard Greig Gillian Kargman Stacia Lamontagne Sonia Martins Evelyn Nantel François O'Neill Gary Sawyer Nicole Metters Kathleen M Friesen Richard W |
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| Affiliation: | Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8. yves_ducgarme@merck.com |
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| 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. |
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