Document Detail


Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity.
MedLine Citation:
PMID:  22209458     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
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
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-12-13
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Dec 
Date Detail:
Created Date:  2012-1-2     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Vernalis (R&D) Ltd, Granta Park, Cambridge CB21 6GB, UK.
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