Title of article
Discovery and Initial SAR of Arylsulfonylpiperazine Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)
Author/Authors
DaQing Sun، نويسنده , , Zhulun Wang، نويسنده , , Yongmei Di، نويسنده , , Juan C. Jaen، نويسنده , , Marc Labelle، نويسنده , , Hong-Ji Ma and Rui Nie، نويسنده , , Shichang Miao، نويسنده , , Athena Sudom، نويسنده , , Liang Tang، نويسنده , , Craig S. Tomooka، نويسنده , , Guan-Hua Tu، نويسنده , , Stefania Ursu، نويسنده , , Nigel Walker، نويسنده , , Xuelei Yan، نويسنده , , Qiuping Ye، نويسنده , , Jay P. Powers and Nigel P.C. Walker، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
3513
To page
3516
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 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11β-HSD1 IC50 = 3 nM).
Keywords
Diabetes , 11?-HSD2 , Hydroxysteroid dehydrogenase , Arylsulfonylpiperazines , metabolic syndrome , 11?-HSD1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799588
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