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rdf:type |
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lifeskim:mentions |
umls-concept:C0020459,
umls-concept:C0026336,
umls-concept:C0031957,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0038760,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243077,
umls-concept:C0442027,
umls-concept:C0470187,
umls-concept:C0909868,
umls-concept:C1527415
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pubmed:issue |
14
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pubmed:dateCreated |
2008-7-22
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pubmed:abstractText |
11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) is the enzyme that converts cortisone to cortisol. Evidence suggests that selective inhibition of 11beta-HSD1 could treat diabetes and metabolic syndrome. Presented herein are the synthesis, structure-activity relationship, and in vivo evaluation of piperazine sulfonamides as 11beta-HSD1 inhibitors. Through modification of our initial lead 5a, we have identified potent and selective 11beta-HSD1 inhibitors such as 13q and 13u with good pharmacokinetic properties.
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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 |
Jul
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BinnunEvaE,
pubmed-author:ChenLihrenL,
pubmed-author:HahmSeungS,
pubmed-author:IpekManusM,
pubmed-author:LiHuan-QiuHQ,
pubmed-author:LiXiangpingX,
pubmed-author:LiZ CZC,
pubmed-author:MansourTarek STS,
pubmed-author:McKewJohn CJC,
pubmed-author:NunezJillJ,
pubmed-author:SaiahEddineE,
pubmed-author:SuriVipinV,
pubmed-author:TobinJamesJ,
pubmed-author:WanZhao-KuiZK,
pubmed-author:XiangJasonJ,
pubmed-author:XingYuzheY,
pubmed-author:YanP SPS
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pubmed:issnType |
Electronic
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pubmed:day |
24
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4068-71
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pubmed:meshHeading |
pubmed-meshheading:18578516-11-beta-Hydroxysteroid Dehydrogenase Type 1,
pubmed-meshheading:18578516-Administration, Oral,
pubmed-meshheading:18578516-Animals,
pubmed-meshheading:18578516-Biological Availability,
pubmed-meshheading:18578516-Cortisone,
pubmed-meshheading:18578516-Disease Models, Animal,
pubmed-meshheading:18578516-Enzyme Inhibitors,
pubmed-meshheading:18578516-Hyperinsulinism,
pubmed-meshheading:18578516-Piperazines,
pubmed-meshheading:18578516-Rats,
pubmed-meshheading:18578516-Sulfonamides
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pubmed:year |
2008
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pubmed:articleTitle |
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
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pubmed:affiliation |
Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, Massachusetts 02140, USA. jxiang@wyeth.com
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pubmed:publicationType |
Journal Article
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