2,3-Diarylthiophenes as selective EP1 receptor antagonists.

@article{Ducharme200523DiarylthiophenesAS,
  title={2,3-Diarylthiophenes as selective EP1 receptor antagonists.},
  author={Yves Ducharme and Marc Blouin and Marie-Claude Carri{\`e}re and Anne Ch{\^a}teauneuf and Bernard C{\^o}t{\'e} and Danielle Denis and R. Frenette and Gillian M. Greig and Stacia Kargman and Sonia Lamontagne and Evelyn Martins and François Nantel and G O'neill and Nicole Sawyer and Kathleen M. Metters and Richard W. Friesen},
  journal={Bioorganic & medicinal chemistry letters},
  year={2005},
  volume={15 4},
  pages={1155-60}
}
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… CONTINUE READING