新型11β-羟基类固醇脱氢酶1型（11β-HSD1）抑制剂芳基磺酰基哌嗪的合成与优化
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
作者信息
Sun Daqing, Wang Zhulun, Cardozo Mario, Choi Rebekah, Degraffenreid Michael, Di Yongmei, He Xiao, Jaen Juan C, Labelle Marc, Liu Jinsong, Ma Ji, Miao Shichang, Sudom Athena, Tang Liang, Tu Hua, Ursu Stefania, Walker Nigel, Yan Xuelei, Ye Qiuping, Powers Jay P
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1522-7. doi: 10.1016/j.bmcl.2008.12.114. Epub 2009 Jan 9.
PMID:19181519
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.
摘要
描述了一系列11β-羟类固醇脱氢酶1（11β-HSD1）的芳基磺酰基哌嗪抑制剂的合成及其构效关系。优化过程迅速产生了强效、选择性且口服生物可利用的抑制剂，这些抑制剂在食蟹猴离体酶抑制模型中显示出疗效。
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