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1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

Authors :
Sandra R. Chaplan
Brian Scott
Michele C. Rizzolio
Joan Pierce
Natalie A. Hawryluk
Mark Seierstad
Leon Chang
J. Guy Breitenbucher
Michelle L. Wennerholm
Mark J. Karbarz
Richard Apodaca
Sandy J. Wilson
John M. Keith
James A. Palmer
Allison Chambers
Michael Webb
Lin Luo
Source :
Bioorganic & Medicinal Chemistry Letters. 24:1280-1284
Publication Year :
2014
Publisher :
Elsevier BV, 2014.

Abstract

A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.

Details

ISSN :
0960894X
Volume :
24
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....dc169c27063de79ede8ba3a615dade39