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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
Structure-guided drug design led to the identification of a class of spirocyclic ureas which potently inhibit human 11beta-HSD1 in vitro. Lead compound 10j was shown to be orally bioavailable in three species, distributed into adipose tissue in the mouse, and its (R) isomer 10j2 was efficacious in a primate pharmacodynamic model.
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BerbaumJenniferJ,
pubmed-author:BiY HYH,
pubmed-author:BrunoJoseph GJG,
pubmed-author:BukhtiyarovYuriY,
pubmed-author:CacatianSalvacion TST,
pubmed-author:ClaremonDavid ADA,
pubmed-author:GuoJoanJ,
pubmed-author:HarrisonRichard KRK,
pubmed-author:KroskyPaula MPM,
pubmed-author:KrukBarbara ABA,
pubmed-author:LindblomPeterP,
pubmed-author:McGeehanGerard MGM,
pubmed-author:McKeeverBrian MBM,
pubmed-author:PanemangaloreReshmaR,
pubmed-author:ScottBoyd BBB,
pubmed-author:SimpsonRobert DRD,
pubmed-author:SinghSuresh BSB,
pubmed-author:TiceColin MCM,
pubmed-author:UndelandK AKA,
pubmed-author:XuZhenrongZ,
pubmed-author:YeYuan-JieYJ,
pubmed-author:ZhaoWeiW,
pubmed-author:ZhaoYiY,
pubmed-author:ZhuangLinghangL
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pubmed:copyrightInfo |
Copyright (c) 2009 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 |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
881-6
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pubmed:meshHeading |
pubmed-meshheading:20064717-11-beta-Hydroxysteroid Dehydrogenase Type 1,
pubmed-meshheading:20064717-Administration, Oral,
pubmed-meshheading:20064717-Animals,
pubmed-meshheading:20064717-Binding Sites,
pubmed-meshheading:20064717-Biological Availability,
pubmed-meshheading:20064717-CHO Cells,
pubmed-meshheading:20064717-Cricetinae,
pubmed-meshheading:20064717-Cricetulus,
pubmed-meshheading:20064717-Drug Design,
pubmed-meshheading:20064717-Humans,
pubmed-meshheading:20064717-Macaca fascicularis,
pubmed-meshheading:20064717-Mice,
pubmed-meshheading:20064717-Rats,
pubmed-meshheading:20064717-Structure-Activity Relationship,
pubmed-meshheading:20064717-Urea
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pubmed:year |
2010
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pubmed:articleTitle |
Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.
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pubmed:affiliation |
Vitae Pharmaceuticals, 502 West Office Center Drive, Fort Washington, PA 19034, USA.
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pubmed:publicationType |
Journal Article,
Comparative Study
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