Structure–activity relationships of 1, 5-biaryl pyrroles as EP 1 receptor antagonists

…, GMP Giblin, RJ Gleave, B Hammond, MP Healy…

文献索引：Hall, Adrian; Atkinson, Stephen; Brown, Susan H.; Chessell, Iain P.; Chowdhury, Anita; Clayton, Nicholas M.; Coleman, Tanya; Giblin, Gerard M.P.; Gleave, Robert J.; Hammond, Beverley; Healy, Mark P.; Johnson, Matthew R.; Michel, Anton D.; Naylor, Alan; Novelli, Riccardo; Spalding, David J.; Tang, Sac P. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 14 p. 3657 - 3662

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被引用次数: 24

摘要

The preliminary SAR of a series of novel 1, 5-biaryl pyrrole EP1 receptor antagonists derived from compound 1 is described. Replacement of the benzyl group of 1 with isosteric groups was investigated. The most effective replacement was found to be the isobutyl group. The cyclopentylmethyl and cyclohexylmethyl groups were also effective benzyl replacements. The cyclohexylmethyl derivative 19 demonstrated the lowest metabolic clearance within ...