Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain

Bioorganic & Medicinal Chemistry Letters
2018.0

Abstract

A novel series of EP4 agonists and antagonists have been identified, and then used to validate their potential in the treatment of inflammatory pain. This paper describes these novel ligands and their activity within a number of pre-clinical models of pain, ultimately leading to the identification of the EP4 partial agonist GSK726701A.

Knowledge Graph

Similar Paper

Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain
Bioorganic & Medicinal Chemistry Letters 2018.0
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile
Bioorganic & Medicinal Chemistry Letters 2016.0
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists
Bioorganic & Medicinal Chemistry Letters 2016.0
Discovery of APD371: Identification of a Highly Potent and Selective CB<sub>2</sub>Agonist for the Treatment of Chronic Pain
ACS Medicinal Chemistry Letters 2017.0
Discovery and Pharmacological Profile of New 1H-Indazole-3-carboxamide and 2H-Pyrrolo[3,4-c]quinoline Derivatives as Selective Serotonin 4 Receptor Ligands
Journal of Medicinal Chemistry 2012.0
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H<sub>4</sub>R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia
Journal of Medicinal Chemistry 2008.0
Discovery and structure–activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor
Bioorganic &amp; Medicinal Chemistry Letters 2010.0
Discovery of Novel 2,5-Dioxoimidazolidine-Based P2X<sub>7</sub>Receptor Antagonists as Constrained Analogues of KN62
Journal of Medicinal Chemistry 2015.0
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology
Bioorganic &amp; Medicinal Chemistry Letters 2008.0
Discovery of new chemical leads for prostaglandin D2 receptor antagonists
Bioorganic &amp; Medicinal Chemistry Letters 2004.0