Identification of novel glycine sulfonamide antagonists for the EP 1 receptor

…, R Blunt, SH Brown, IP Chessell, A Chowdhury…

文献索引：McKeown, Stephen C.; Hall, Adrian; Blunt, Richard; Brown, Susan H.; Chessell, Iain P.; Chowdhury, Anita; Giblin, Gerard M.P.; Healy, Mark P.; Johnson, Matthew R.; Lorthioir, Olivier; Michel, Anton D.; Naylor, Alan; Lewell, Xiao; Roman, Shilina; Watson, Stephen P.; Winchester, Wendy J.; Wilson, Richard J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1750 - 1754

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被引用次数: 17

摘要

A high-throughput screen targeting the EP1 receptor identified non-acidic glycine sulfonamide derivative 2a with a pKi of 6.2. Analogue synthesis allowed a thorough investigation of the structure–activity relationship (SAR) and led to a 100-fold increase in recombinant potency.