title: Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
abstract: We describe the discovery and optimization of a novel series of benzofuran EP(1) antagonists, leading to the identification of 26d, a novel nonacidic EP(1) antagonist which demonstrated efficacy in preclinical models of chronic inflammatory pain.
authors.affiliation: Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.
authors.forename: Amanda C
authors.initials: AC
authors.lastname: Allan
authors.forename: Andy
authors.initials: A
authors.lastname: Billinton
authors.forename: Susan H
authors.initials: SH
authors.lastname: Brown
authors.forename: Anita
authors.initials: A
authors.lastname: Chowdhury
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Eatherton
authors.forename: Charlotte
authors.initials: C
authors.lastname: Fieldhouse
authors.forename: Gerard M P
authors.initials: GM
authors.lastname: Giblin
authors.forename: Paul
authors.initials: P
authors.lastname: Goldsmith
authors.forename: Adrian
authors.initials: A
authors.lastname: Hall
authors.forename: David N
authors.initials: DN
authors.lastname: Hurst
authors.forename: Alan
authors.initials: A
authors.lastname: Naylor
authors.forename: D Anthony
authors.initials: DA
authors.lastname: Rawlings
authors.forename: Mairi
authors.initials: M
authors.lastname: Sime
authors.forename: Tiziana
authors.initials: T
authors.lastname: Scoccitti
authors.forename: Pamela J
authors.initials: PJ
authors.lastname: Theobald
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001572:Benzofurans / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002460:Cell Line; D004195:Disease Models, Animal; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D010146:Pain / Q000188:drug therapy; D051381:Rats; D058306:Receptors, Prostaglandin E, EP1 Subtype / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D001572:Benzofurans; D058306:Receptors, Prostaglandin E, EP1 Subtype; C105430:benzofuran