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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2002-8-22
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pubmed:abstractText |
Novel antidiabetic arylsulfonamidothiazoles are presented that exert action through selective inhibition of the 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) enzyme, thereby attenuating hepatic gluconeogenesis. The diethylamide derivative 2a was shown to potently inhibit human 11beta-HSD1 (IC(50) = 52 nM), whereas the N-methylpiperazinamide analogue 2b only inhibited murine 11beta-HSD1 (IC(50) = 96 nM). Both compounds showed >200-fold selectivity over human and murine 11beta-HSD2. 2b was subsequently shown to reduce glucose levels in diabetic KKA(y) mice, substantiating the 11beta-HSD1 enzyme as a target for the treatment of type 2 diabetes.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AbrahmsénLarsL,
pubmed-author:AlbertsPeterisP,
pubmed-author:AxelssonKentK,
pubmed-author:BarfTjeerdT,
pubmed-author:EdlingNaimieN,
pubmed-author:EmondRikardR,
pubmed-author:EngblomLarsL,
pubmed-author:HäggströmCharlottaC,
pubmed-author:KurzGuidoG,
pubmed-author:LarwoodVivienneV,
pubmed-author:MosialouErifiliE,
pubmed-author:NygrenAlfA,
pubmed-author:OhmanBirgittaB,
pubmed-author:OlssonRolfR,
pubmed-author:Rönquist-NiiYukoY,
pubmed-author:VallgårdaJerkJ
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pubmed:issnType |
Print
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pubmed:day |
29
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pubmed:volume |
45
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|
pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3813-5
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
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pubmed:year |
2002
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pubmed:articleTitle |
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
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pubmed:affiliation |
Department of Medicinal Chemistry, Biovitrum, Box 6443, SE-751 37, Uppsala, Sweden. tjeerd.barf@biovitrum.com
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pubmed:publicationType |
Journal Article
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