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ID: ALA1141865

Journal: Bioorg Med Chem Lett

Title: Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.

Authors: Gu X, Dragovic J, Koo GC, Koprak SL, LeGrand C, Mundt SS, Shah K, Springer MS, Tan EY, Thieringer R, Hermanowski-Vosatka A, Zokian HJ, Balkovec JM, Waddell ST.

Abstract: Replacement of the pentyl chain on our original bicyclo[2.2.2]octyltriazole leads 1 and 2 has led to the discovery that heteroaryl substituted bicyclo[2.2.2]octyltriazoles are potent and selective 11beta-hydroxysteroid dehydrogenase type I (11beta-HSD1) inhibitors with excellent pharmacokinetic profiles.

CiteXplore: 16185866

DOI: 10.1016/j.bmcl.2005.08.052