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Bioorg Med Chem Lett. 2009 Mar 1;19(5):1522-7. doi: 10.1016/j.bmcl.2008.12.114. Epub 2009 Jan 9.

Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).

Abstract

The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11beta-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model.

PMID:
19181519
DOI:
10.1016/j.bmcl.2008.12.114
[Indexed for MEDLINE]

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