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