Hall Adrian, Atkinson Stephen, Brown Susan H, Chessell Iain P, Chowdhury Anita, Giblin Gerard M P, Goldsmith Paul, Healy Mark P, Jandu Karamjit S, Johnson Matthew R, Michel Anton D, Naylor Alan, Sweeting Jennifer A
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1200-5. doi: 10.1016/j.bmcl.2006.12.021. Epub 2006 Dec 12.
Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding efficiency indices.
在一系列先前描述的1,5-二芳基吡咯EP1受体拮抗剂中替换羧酸基团,导致发现了各种新型非酸性拮抗剂。几种类似物表现出高结合亲和力和高结合效率指数。