1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid deriv...
Basic Information
ID: ALA1144577
Journal: Bioorg Med Chem Lett
Title: 1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Authors: Hall A, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Hammond B, Healy MP, Johnson MR, Metcalf A, Michel AD, Naylor A, Novelli R, Spalding DJ, Sweeting J, Winyard L.
Abstract: Herein we describe the SAR of 1,5-biaryl pyrrole derivatives, with substituents in the 6-position of the benzoic acid moiety, as EP(1) receptor antagonists. Substitution at this position was well tolerated and led to the identification of several analogues with high affinity for the EP(1) receptor that displayed good efficacy in the established FCA model of inflammatory pain. Furthermore, several analogues were prepared which combined substitution at the 5- and 6-positions as well as derivatives with an aromatic ring fused to the 5- and 6-positions.
CiteXplore: 17175160
DOI: 10.1016/j.bmcl.2006.11.059
Patent ID: ┄