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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase

Authors :
Raymond Rynberg
Sandy J. Wilson
William M. Jones
Michele C. Rizzolio
Mark Seierstad
Lin Luo
John M. Keith
Michelle Wennerholm
Joan Pierce
Michael Webb
Sean Brown
James A. Palmer
Sandra R. Chaplan
Mark J. Karbarz
Brian Scott
Leon Chang
J. Guy Breitenbucher
Source :
Bioorganic & Medicinal Chemistry Letters. 24:737-741
Publication Year :
2014
Publisher :
Elsevier BV, 2014.

Abstract

A series of mechanism based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty acid ethanolamides [FAAs: anandamide (AEA), oleoyl ethanolamide (OEA) and palmitoyl ethanolamide (PEA)], and was moderately 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.....c4908988252b5adc440f435416fadbcc
Full Text :
https://doi.org/10.1016/j.bmcl.2013.12.113