2014 Jan 31. pii: S0960-894X(14)00094-8. doi: 10.1016/j.bmcl.2014.01.064. [Epub ahead of print]
1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.
Keith JM1, Hawryluk N2, Apodaca RL2, Chambers A2, Pierce JM2, Seierstad M2, Palmer JA2, Webb M2, Karbarz MJ2, Scott BP2, Wilson SJ2, Luo L2,Wennerholm ML2, Chang L2, Rizzolio M2, Chaplan SR2, Breitenbucher JG2.
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.
Copyright © 2014 Elsevier Ltd. All rights reserved.
Copyright © 2014 Elsevier Ltd. All rights reserved.
KEYWORDS:
Analgesia, Crystal structure, Endo-cannabinoids, Enzymes, Fatty acid amide hydrolase (FAAH)
- PMID:
- 24513048
- [PubMed – as supplied by publisher]
