Discovery of GSK345931A: An EP 1 receptor antagonist with efficacy in preclinical models of inflammatory pain

…, A Naylor, DA Rawlings, T Scoccitti, AW Wilson…

文献索引：Hall, Adrian; Brown, Susan H.; Budd, Christopher; Clayton, Nicholas M.; Giblin, Gerard M.P.; Goldsmith, Paul; Hayhow, Thomas G.; Hurst, David N.; Naylor, Alan; Anthony Rawlings; Scoccitti, Tiziana; Wilson, Alexander W.; Winchester, Wendy J. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 497 - 501

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被引用次数: 18

摘要

Herein we describe the medicinal chemistry programme to identify a potential back-up compound to the EP1 receptor antagonist GW848687X. This work started with the lipophilic 1, 2-biaryl benzene derivative 4 which displayed molecular weight of 414.9 g/mol and poor in vivo metabolic stability in the rat and resulted in the identification of compound 7i (GSK345931A) which demonstrated good metabolic stability in the rat and lower ...