Yuping Zhu, S. Olson, D. Graham
Jun 1, 2008
Citations
0
Influential Citations
39
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-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.