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Bioorg Med Chem Lett. 2012 Jan 15;22(2):901-6. doi: 10.1016/j.bmcl.2011.12.032. Epub 2011 Dec 13.

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

Author information

1
Vernalis (R&D) Ltd, Granta Park, Cambridge CB21 6GB, UK. s.roughley@vernalis.com

Abstract

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.

PMID:
22209458
DOI:
10.1016/j.bmcl.2011.12.032
[Indexed for MEDLINE]

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