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
Related Documents :
1691218 - Laboratory and field performance of consumer bait products for german cockroach (dictyo...
3980328 - Bactericidal effects of amoxycillin/clavulanic acid and ticarcillin/clavulanic acid in ...
8099958 - In-vitro permeability to salicylic acid of human, rodent, and shed snake skin.
3144548 - Rate of bactericidal activity for branhamella catarrhalis of fleroxacin compared with t...
15158478 - Quantitative gas chromatography/mass spectrometry determination of c-mannosylation of t...
14986948 - Boric acid catalyzed chemoselective esterification of alpha-hydroxycarboxylic acids.
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.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid recept...
Next Document:  Synthesis of 5-benzyl-2-phenylpyrazolo[1,5-a]pyrazin-4,6(5H,7H)-dione derivatives and discovery of a...