632628-04-7Relevant articles and documents
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives
Hall, Adrian,Brown, Susan H.,Chessell, Iain P.,Chowdhury, Anita,Clayton, Nicholas M.,Coleman, Tanya,Giblin, Gerard M.P.,Hammond, Beverley,Healy, Mark P.,Johnson, Matthew R.,Metcalf, Ann,Michel, Anton D.,Naylor, Alan,Novelli, Riccardo,Spalding, David J.,Sweeting, Jennifer,Winyard, Lisa
, p. 916 - 920 (2007/10/03)
Herein we describe the SAR of 1,5-biaryl pyrrole derivatives, with substituents in the 6-position of the benzoic acid moiety, as EP1 receptor antagonists. Substitution at this position was well tolerated and led to the identification of several analogues with high affinity for the EP1 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.