| Literature DB >> 24433863 |
John M Keith1, William M Jones2, Joan M Pierce2, Mark Seierstad2, James A Palmer2, Michael Webb2, Mark J Karbarz2, Brian P Scott2, Sandy J Wilson2, Lin Luo2, Michelle L Wennerholm2, Leon Chang2, Sean M Brown2, Michele Rizzolio2, Raymond Rynberg2, Sandra R Chaplan2, J Guy Breitenbucher2.
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.Entities:
Keywords: Covalent inhibitor; FAAH; Hydrolase; Spirocycles
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Year: 2014 PMID： 24433863 DOI： 10.1016/j.bmcl.2013.12.113
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823