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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2011-4-4
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pubmed:abstractText |
Starting from a series of ureas that were determined to be mechanism-based inhibitors of FAAH, several spirocyclic ureas and lactams were designed and synthesized. These efforts identified a series of novel, noncovalent FAAH inhibitors with in vitro potency comparable to known covalent FAAH inhibitors. The mechanism of action for these compounds was determined through a combination of SAR and co-crystallography with rat FAAH.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:CarlsonTimothy JTJ,
pubmed-author:ConnorsRichardR,
pubmed-author:GuimaraesCrisC,
pubmed-author:GustinDarin JDJ,
pubmed-author:HedbergChristineC,
pubmed-author:KayserFrankF,
pubmed-author:Lester-ZeinerDiannaD,
pubmed-author:LiYihongY,
pubmed-author:LindstromMichelleM,
pubmed-author:MaZhihuaZ,
pubmed-author:MelezaCesarC,
pubmed-author:MinXiaoshanX,
pubmed-author:PorterAmy CAC,
pubmed-author:WangZhulunZ,
pubmed-author:XiaoShouhuaS,
pubmed-author:XuGuifenG
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pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2492-6
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pubmed:meshHeading |
pubmed-meshheading:21392988-Amidohydrolases,
pubmed-meshheading:21392988-Animals,
pubmed-meshheading:21392988-Binding Sites,
pubmed-meshheading:21392988-Computer Simulation,
pubmed-meshheading:21392988-Crystallography, X-Ray,
pubmed-meshheading:21392988-Enzyme Inhibitors,
pubmed-meshheading:21392988-Humans,
pubmed-meshheading:21392988-Lactams,
pubmed-meshheading:21392988-Rats,
pubmed-meshheading:21392988-Spiro Compounds,
pubmed-meshheading:21392988-Structure-Activity Relationship,
pubmed-meshheading:21392988-Urea
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pubmed:year |
2011
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pubmed:articleTitle |
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
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pubmed:affiliation |
Department of Chemistry, Amgen Inc., South San Francisco, 1120 Veterans Blvd., South San Francisco, CA 94080, USA. dgustin@amgen.com
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pubmed:publicationType |
Journal Article
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