Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists

Amanda C. Allan,Andy Billinton,Susan H. Brown,Anita Chowdhury,Andrew J. Eatherton,Charlotte Fieldhouse,Gerard M.P. Giblin,Paul Goldsmith,Adrian Hall,David N. Hurst,Alan Naylor,D. Anthony Rawlings,Mairi Sime,Tiziana Scoccitti,Pamela J. Theobald

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

We describe the discovery and optimization of a novel series of benzofuran EP1 antagonists, leading to the identification of 26d, a novel nonacidic EP1 antagonist which demonstrated efficacy in preclinical models of chronic inflammatory pain.

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关键词

EP1 antagonist,Pain,CNS penetration,Scaffold hopping

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