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ID: ALA1145647

Journal: Bioorg Med Chem Lett

Title: Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Authors: Zhu Y, Olson SH, Graham D, Patel G, Hermanowski-Vosatka A, Mundt S, Shah K, Springer M, Thieringer R, Wright S, Xiao J, Zokian H, Dragovic J, Balkovec JM.

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.

CiteXplore: 18440812

DOI: 10.1016/j.bmcl.2008.04.014