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

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 prof...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-12, Vol.15 (23), p.5266-5269
Main Authors: Gu, Xin, Dragovic, Jasminka, Koo, Gloria C, Koprak, Sam L, LeGrand, Cheryl, Mundt, Steven S, Shah, Kashmira, Springer, Marty S, Tan, Eugene Y, Thieringer, Rolf, Hermanowski-Vosatka, Anne, Zokian, Hratch J, Balkovec, James M, Waddell, Sherman T
Format: Article
Language:English
Subjects:
11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors
Animals
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - therapeutic use
Humans
Metabolic Syndrome - drug therapy
Mice
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - therapeutic use
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Summary: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.
ISSN:0960-894X