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Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Nov2010, Vol. 20 Issue 22, p6725-6729. 5p. - Publication Year :
- 2010
-
Abstract
- Abstract: Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 9a with an IC50 of 15.2nM 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. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 20
- Issue :
- 22
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 54482668
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.08.142