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

…, Z Wang, Y Di, JC Jaen, M Labelle, J Ma, S Miao…

文献索引：Sun, Daqing; Wang, Zhulun; Di, Yongmei; Jaen, Juan C.; Labelle, Marc; Ma, Ji; Miao, Shichang; Sudom, Athena; Tang, Liang; Tomooka, Craig S.; Tu, Hua; Ursu, Stefania; Walker, Nigel; Yan, Xuelei; Ye, Qiuping; Powers, Jay P. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 12 p. 3513 - 3516

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被引用次数: 38

摘要

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= 3nM).