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Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Authors:Aster Susan D  Graham Donald W  Kharbanda Divya  Patel Gool  Ponpipom Mitree  Santorelli Gina M  Szymonifka Michael J  Mundt Steven S  Shah Kashmira  Springer Marty S  Thieringer Rolf  Hermanowski-Vosatka Anne  Wright Samuel D  Xiao Jianying  Zokian Hratch  Balkovec James M
Institution:

aDepartment of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA

bDepartment of Cardiovascular Disease, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA

Abstract:3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.
Keywords:11β-Hydroxysteroid dehydrogenase  Metabolic syndrome  Bis-aryl triazoles
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