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Bioorg Med Chem Lett. 2011 Jan 15;21(2):734-7. doi: 10.1016/j.bmcl.2010.11.118. Epub 2010 Dec 3.

The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.

Author information

1
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Hwy., Kirkland, Québec, Canada H9H 3L1. lianhai_li@merck.com

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.

PMID:
21208803
DOI:
10.1016/j.bmcl.2010.11.118
[Indexed for MEDLINE]

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