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2005
Thiophene derivatives
R 0090
2,3-Diarylthiophenes as Selective EP1 Receptor Antagonists. — The synthesis of
antagonists rely heavily on Stille and Suzuki coupling reactions of the required
26- 060 the
building blocks. The results of a structure—activity relationship study directed towards
the optimization of analogues of a prototypical EP1 receptor antagonist in terms of EP1
binding affinity, selectivity, functional activity, and pharmacokinetics are disclosed.
Compounds (VIa), (VII), and (XI) are identified as antagonists exhibiting high affinity
for the human EP1 receptor and a selectivity greater than 100-fold against the EP2, EP3,
EP4, DP, FP, and IP receptors and greater than 25-fold vs. the TP receptor. These antagonists show good pharmacokinetic behavior and reveal significant differences in the
brain-blood distribution. — (DUCHARME*, Y.; et al.; Bioorg. Med. Chem. Lett. 15
(2005) 4, 1155-1160; Merck Frosst Cent. Ther. Res., Pointe-Claire-Dorval,
Que. H9R 4P8, Can.; Eng.) — H. Hoennerscheid
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