Bioorganic & Medicinal Chemistry Letters 2012-01-15

Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.

Stephen D Roughley, Helen Browne, Alba T Macias, Karen Benwell, Teresa Brooks, Jalanie D'Alessandro, Zoe Daniels, Sarah Dugdale, Geraint Francis, Ben Gibbons, Terance Hart, Timothy Haymes, Guy Kennett, Sean Lightowler, Natalia Matassova, Howard Mansell, Angela Merrett, Anil Misra, Anthony Padfield, Rachel Parsons, Robert Pratt, Alan Robertson, Heather Simmonite, Kiri Tan, Steven B Walls, Melanie Wong

文献索引：Bioorg. Med. Chem. Lett. 22(2) , 901-6, (2012)

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摘要

We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration of in vivo dose-dependant FAAH inhibition in an anandamide-loading study in rats.Copyright © 2011 Elsevier Ltd. All rights reserved.