Linked Life Data

12190302

Source:http://linkedlifedata.com/resource/pubmed/id/12190302

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pubmed-article:12190302pubmed:abstractTextNovel 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.lld:pubmed
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pubmed-article:12190302pubmed:articleTitleArylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.lld:pubmed
pubmed-article:12190302pubmed:affiliationDepartment of Medicinal Chemistry, Biovitrum, Box 6443, SE-751 37, Uppsala, Sweden. tjeerd.barf@biovitrum.comlld:pubmed
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