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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-12-24
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pubmed:abstractText |
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11?-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:CailleSebS,
pubmed-author:DeGraffenreidMichaelM,
pubmed-author:Gonzalez-Lopez de TurisoFelixF,
pubmed-author:HungateRandallR,
pubmed-author:JaenJuan CJC,
pubmed-author:JiangBenB,
pubmed-author:JulianLisa DLD,
pubmed-author:KaizermanJacobJ,
pubmed-author:KellyRonR,
pubmed-author:McMinnDustin LDL,
pubmed-author:PowersJay PJP,
pubmed-author:RewYosupY,
pubmed-author:SudomAthenaA,
pubmed-author:SunDaqingD,
pubmed-author:TuHuaH,
pubmed-author:UrsuStefaniaS,
pubmed-author:WalkerNigelN,
pubmed-author:WangZhulunZ,
pubmed-author:WillcocksonMarenM,
pubmed-author:YanXueleiX,
pubmed-author:YeQiupingQ
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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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 |
405-10
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pubmed:meshHeading |
pubmed-meshheading:21093258-11-beta-Hydroxysteroid Dehydrogenase Type 1,
pubmed-meshheading:21093258-Administration, Oral,
pubmed-meshheading:21093258-Animals,
pubmed-meshheading:21093258-Benzamides,
pubmed-meshheading:21093258-Binding Sites,
pubmed-meshheading:21093258-Crystallography, X-Ray,
pubmed-meshheading:21093258-Enzyme Inhibitors,
pubmed-meshheading:21093258-Humans,
pubmed-meshheading:21093258-Macaca fascicularis,
pubmed-meshheading:21093258-Microsomes, Liver,
pubmed-meshheading:21093258-Rats,
pubmed-meshheading:21093258-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11?-HSD1 inhibitors.
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pubmed:affiliation |
Amgen Inc, 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. daqings@amgen.com
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pubmed:publicationType |
Journal Article
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