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The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.
Li, Lianhai; Mathieu, Marie-Claude; Denis, Danielle; Therien, Alex G; Wang, Zhaoyin.
Affiliation
  • Li L; Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Hwy., Kirkland, Québec, Canada H9H 3L1. lianhai_li@merck.com
Bioorg Med Chem Lett ; 21(2): 734-7, 2011 Jan 15.
Article in En | MEDLINE | ID: mdl-21208803
ABSTRACT
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiophenes / Receptors, Prostaglandin E, EP4 Subtype Type of study: Diagnostic_studies Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiophenes / Receptors, Prostaglandin E, EP4 Subtype Type of study: Diagnostic_studies Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article