title: 3,4-Disubstituted indole acylsulfonamides: a novel series of potent and selective human EP3 receptor antagonists.
abstract: A series of potent and selective EP(3) receptor antagonists are described. Utilizing a pharmacophore model developed for the EP(3) receptor, a series of 3,4-disubstituted indoles were shown to be high affinity ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors and are potent antagonists in functional assays.
authors.affiliation: Medicinal Chemistry Department, deCODE Chemistry, Inc, Woodridge, IL 60517, USA.
authors.forename: Nian
authors.initials: N
authors.lastname: Zhou
authors.forename: Wayne
authors.initials: W
authors.lastname: Zeller
authors.forename: Michael
authors.initials: M
authors.lastname: Krohn
authors.forename: Herb
authors.initials: H
authors.lastname: Anderson
authors.forename: Jun
authors.initials: J
authors.lastname: Zhang
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Onua
authors.forename: Alex S
authors.initials: AS
authors.lastname: Kiselyov
authors.forename: Jose
authors.initials: J
authors.lastname: Ramirez
authors.forename: Gułrún
authors.initials: G
authors.lastname: Halldorsdottir
authors.forename: Thornorkell
authors.initials: T
authors.lastname: Andrésson
authors.forename: Mark E
authors.initials: ME
authors.lastname: Gurney
authors.forename: Jasbir
authors.initials: J
authors.lastname: Singh
mesh_terms: D006801:Humans; D007211:Indoles; D008024:Ligands; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058308:Receptors, Prostaglandin E, EP3 Subtype; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D007211:Indoles; D008024:Ligands; C545647:PTGER3 protein, human; D018078:Receptors, Prostaglandin E; D058308:Receptors, Prostaglandin E, EP3 Subtype; D013449:Sulfonamides