title: Novel methylene-linked heterocyclic EP1 receptor antagonists.
abstract: We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP(1) receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investigation of replacements for the methylene linker uncovered disparate SAR in the thiazole and pyridine series.
authors.affiliation: Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom. adrian.2.hall@gsk.com
authors.forename: Adrian
authors.initials: A
authors.lastname: Hall
authors.forename: Rino A
authors.initials: RA
authors.lastname: Bit
authors.forename: Susan H
authors.initials: SH
authors.lastname: Brown
authors.forename: Anita
authors.initials: A
authors.lastname: Chowdhury
authors.forename: Gerard M P
authors.initials: GM
authors.lastname: Giblin
authors.forename: David N
authors.initials: DN
authors.lastname: Hurst
authors.forename: Ian R
authors.initials: IR
authors.lastname: Kilford
authors.forename: Xiao
authors.initials: X
authors.lastname: Lewell
authors.forename: Alan
authors.initials: A
authors.lastname: Naylor
authors.forename: Tiziana
authors.initials: T
authors.lastname: Scoccitti
mesh_terms: D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship
chemical_list: D006571:Heterocyclic Compounds; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype