3,4-Disubstituted indole acylsulfonamides: a novel series of potent and selective human EP3 receptor antagonists.
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.
Zhou
Nian
N
Medicinal Chemistry Department, deCODE Chemistry, Inc, Woodridge, IL 60517, USA.
Zeller
Wayne
W
Krohn
Michael
M
Anderson
Herb
H
Zhang
Jun
J
Onua
Emmanuel
E
Kiselyov
Alex S
AS
Ramirez
Jose
J
Halldorsdottir
Gułrún
G
Andrésson
Thornorkell
T
Gurney
Mark E
ME
Singh
Jasbir
J
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
D007211:Indoles; D008024:Ligands; C545647:PTGER3 protein, human; D018078:Receptors, Prostaglandin E; D058308:Receptors, Prostaglandin E, EP3 Subtype; D013449:Sulfonamides