✦ LIBER ✦

The identification of substituted benzothiophene derivatives as PGE2 subtype 4 receptor antagonists: From acid to non-acid

✍ Scribed by Lianhai Li; Marie-Claude Mathieu; Danielle Denis; Alex G. Therien; Zhaoyin Wang

Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 495 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.11.118

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✦ Synopsis

We disclose herein our preliminary SAR study on the identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists. A potent EP(4) antagonist 6a (K(i)=1.4nM with 10% HSA) was identified. Furthermore, we found that an acidic group was not essential for the EP(4) antagonizing activity in the series and neutral replacements were identified. This opens a new direction for future EP(4) antagonist design.

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