AI Article Synopsis
- - Replacement of the pentyl chain in bicyclo[2.2.2]octyltriazole derivatives 1 and 2 resulted in new compounds with enhanced properties.
- - The modified heteroaryl substituted bicyclo[2.2.2]octyltriazoles were found to be strong and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I (11beta-HSD1).
- - These new compounds also demonstrated excellent pharmacokinetic profiles, indicating potential for effective therapeutic use.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2005.08.052 | DOI Listing |
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