Title of article
Phenylcyclobutyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I
Author/Authors
Yuping Zhu، نويسنده , , Steven H. Olson، نويسنده , , Donald Graham، نويسنده , , Gool Patel، نويسنده , , Anne Hermanowski-Vosatka، نويسنده , , Steven Mundt، نويسنده , , Kashmira Shah، نويسنده , , Marty Springer، نويسنده , , Rolf Thieringer، نويسنده , , Samuel Wright، نويسنده , , Jianying Xiao، نويسنده , , Hratch Zokian، نويسنده , , Jasminka Dragovic، نويسنده , , James M. Balkovec، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
3412
To page
3416
Abstract
3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). These were active both in vitro and in an in vivo mouse pharmacodynamic (PD) model. Fluorine substitution of the cyclobutane ring improved the pharmacokinetic profile significantly. The synthesis and structure–activity relationships are presented.
Keywords
11?-HSD1 , metabolic syndrome , Phenylcyclobutyl triazole
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799570
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