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Bioorg Med Chem Lett. 2008 Jun 15;18(12):3513-6. doi: 10.1016/j.bmcl.2008.05.025. Epub 2008 May 10.

Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).

Author information

1
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. daqings@amgen.com

Abstract

High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11beta-Hydroxysteroid Dehydrogenase Type 1 (11beta-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11beta-HSD1 IC(50)=3nM).

PMID:
18511278
DOI:
10.1016/j.bmcl.2008.05.025
[Indexed for MEDLINE]

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