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Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase

Authors :
James A. Palmer
Michael Webb
Michelle Wennerholm
Pattabiraman Kanaka
Mark J. Karbarz
Sandy J. Wilson
Sandra R. Chaplan
Chui-Se Tham
Lin Luo
Brian Scott
Mark Seierstad
J. Guy Breitenbucher
Wei Xiao
Jiejun Wu
Richard Apodaca
John M. Keith
Sean Brown
Source :
Bioorganic & Medicinal Chemistry Letters. 18:4838-4843
Publication Year :
2008
Publisher :
Elsevier BV, 2008.

Abstract

A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.

Details

ISSN :
0960894X
Volume :
18
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....52fa7be7ec1200469cf9e6da14674efa
Full Text :
https://doi.org/10.1016/j.bmcl.2008.07.081