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

  • Bioorg Med Chem Lett. 2008 Jun 15;18(12):3513-6. doi: 10.1016/j.bmcl.2008.05.025.
Daqing Sun  1 ,  Zhulun Wang ,  Yongmei Di ,  Juan C Jaen ,  Marc Labelle ,  Ji Ma ,  Shichang Miao ,  Athena Sudom ,  Liang Tang ,  Craig S Tomooka ,  Hua Tu ,  Stefania Ursu ,  Nigel Walker ,  Xuelei Yan ,  Qiuping Ye ,  Jay P Powers
Affiliations
  • 1. Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. [email protected]
PMID: 18511278 DOI: 10.1016/j.bmcl.2008.05.025
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).

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