Title of article :
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11β-HSD1: Novel therapeutic agents for the treatment of metabolic syndrome
Author/Authors :
Xin Gu، نويسنده , , Jasminka Dragovic، نويسنده , , Gloria C. Koo، نويسنده , , Sam L. Koprak، نويسنده , , Cheryl LeGrand، نويسنده , , Steven S. Mundt، نويسنده , , Kashmira Shah، نويسنده , , Marty S. Springer، نويسنده , , Eugene Y. Tan، نويسنده , , Rolf Thieringer، نويسنده , , Anne Hermanowski-Vosatka، نويسنده , , Hratch J. Zokian، نويسنده , , James M. Balkovec، نويسنده , , Sherman T. Waddell، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
Pages :
4
From page :
5266
To page :
5269
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 11β-hydroxysteroid dehydrogenase type I (11β-HSD1) inhibitors with excellent pharmacokinetic profiles.
Keywords :
11?-Hydroxysteroid dehydrogenase type I , 11?-HSD1 , 11?-HSD2 , glucocorticoids , Cortisone , cortisol , Heterocycle , Oxadiazole , triazole , Pharmacokinectics , Pharmacodynamic assay , Metabolic syndrome , imidazole
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2005
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
796170
Link To Document :
https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=796170
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