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 ,
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.
