1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase |
| |
| Institution: | 1. Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari “Aldo Moro”, Via Orabona 4, 70125 Bari, Italy;2. Pharmaceutical and Medicinal Chemistry, Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), PO Box 15 11 50, D-66041 Saarbrücken, Germany;1. Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305, USA;2. School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia;3. Department of Pharmaceutical Sciences, University of Florence, Via U. Schiff, 650019 Polo Scientifico Sesto Fiorentino, Italy;4. Department of Pharmacy, University of Pisa, Via Bonanno 6, 56127 Pisa, Italy;5. Faculty of Health Sciences, The University of Sydney, Sydney, NSW 2006, Australia |
| |
| 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. |
| |
| Keywords: | Fatty acid amide hydrolase (FAAH) Enzymes Crystal structure Endo-cannabinoids Analgesia |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
