| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371640 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 9a with an IC50 of 15.2 nM against human 11β-HSD1 in adipocytes. Optimization for increased adipocyte potency, metabolic stability and selectivity afforded 11k and 11l, both of which were >25% orally bioavailable in rat.
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Related Topics
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Authors
Colin M. Tice, Wei Zhao, Paula M. Krosky, Barbara A. Kruk, Jennifer Berbaum, Judith A. Johnson, Yuri Bukhtiyarov, Reshma Panemangalore, Boyd B. Scott, Yi Zhao, Joseph G. Bruno, Lamont Howard, Jennifer Togias, Yuan-Jie Ye, Suresh B. Singh,