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Bioorg Med Chem Lett ; 19(1): 123-6, 2009 Jan 01.
Article in English | MEDLINE | ID: mdl-19022669

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.


Subject(s)
Receptors, Prostaglandin E/antagonists & inhibitors , Sulfonamides/chemical synthesis , Humans , Indoles , Ligands , Receptors, Prostaglandin E, EP3 Subtype , Structure-Activity Relationship , Sulfonamides/pharmacology
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