Discovery of a novel indole series of EP 1 receptor antagonists by scaffold hopping

A Hall, A Billinton, SH Brown, A Chowdhury…

文献索引：Hall, Adrian; Billinton, Andy; Brown, Susan H.; Chowdhury, Anita; Giblin, Gerard M.P.; Goldsmith, Paul; Hurst, David N.; Naylor, Alan; Patel, Sadhana; Scoccitti, Tiziana; Theobald, Pamela J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 8 p. 2684 - 2690

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被引用次数: 14

摘要

We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.