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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6725-9. doi: 10.1016/j.bmcl.2010.08.142. Epub 2010 Sep 7.

Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1.

Author information

1
Vitae Pharmaceuticals, 502 W. Office Center Drive, Fort Washington, PA 19034, USA. ctice@vitaerx.com

Abstract

Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 9a with an IC(50) 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.

PMID:
20864344
DOI:
10.1016/j.bmcl.2010.08.142
[Indexed for MEDLINE]

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