含金刚烷的11β-羟基类固醇脱氢酶1抑制剂的杂环化合物的合成与生物学评价
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.
作者信息
Yeh Vince S C, Patel Jyoti R, Yong Hong, Kurukulasuriya Ravi, Fung Steven, Monzon Katina, Chiou William, Wang Jiahong, Stolarik Deanne, Imade Hovis, Beno David, Brune Michael, Jacobson Peer, Sham Hing, Link J T
机构信息
Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, AP-10,304B, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 2006 Oct 15;16(20):5414-9. doi: 10.1016/j.bmcl.2006.07.055. Epub 2006 Aug 8.
A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.
一系列代谢稳定的金刚烷酰胺11β-羟基类固醇脱氢酶1（11β-HSD1）抑制剂已被合成并进行了生物学评估。这些化合物表现出优异的11β-HSD1活性、11β-HSD2选择性以及良好的药代动力学和药效学特性。
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