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有机化学
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有机化学 ›› 2005, Vol. 25 ›› Issue (07): 865-868. 上一篇    下一篇

研究简报

硫代氢化脲嘧啶的合成及其对Hill反应的抑制活性

姚昌盛1，朱晔容2，胡方中1，邹小毛1，朱有全1
高颖1，王勇2 杨华铮*,1   

  1. (1南开大学元素有机化学研究所 元素有机化学国家重点实验室 天津 300071)
    (2南开大学生命科学院 天津 300071)
  • 收稿日期:2004-09-27 修回日期:2005-01-27 发布日期:2005-06-30
  • 通讯作者: YANG Hua-Zheng

Synthesis of Thiohydrouracils and Their Inhibitory Activity againstHill Reaction

YAO Chang-Sheng1,ZHU Ye-Rong2,HU Fang-Zhong1,ZOU Xiao-Mao1
ZHU You-Quan1,GAO Ying1,WANG Yong2,YANG Hua-Zheng*,1   

  1. (1 Institute of Elemento-Organic Chemistry, State Key Laboratory of Elemento-Organic Chemis-try,
    Nankai University, Tianjin 300071)
    (2 College of Life Sci-ence, Nankai University, Tianjin 300071)
  • Received:2004-09-27 Revised:2005-01-27 Published:2005-06-30
  • Contact: 杨华铮

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1226

被引次数

4

为了寻找高活性的Hill反应抑制剂, 以β-氨基丙酸为原料, 经过四步反应, 合成了一系列未经文献报道的3-取代硫代氢化脲嘧啶. 所有新化合物的结构均经过1H NMR, IR和元素分析证. 初步的生物活性测试表明, 所合成的化合物能有效地抑制Hill反应, 如化合物 5j 有很高的抑制活性(IC50＝0.82 g•mL－1).

关键词: 硫代氢化脲嘧啶, 合成, 抑制, Hill反应

In order to find highly active inhibitors of Hill reaction, a series of thiohydrouracil derivatives have been synthesized by a four-step synthetic route. The structures of all compounds were confirmed by elemental analysis, 1H NMR and IR spectra. Preliminary bioassay showed that these compounds could inhibit Hill reaction effectively, for example, compound 5j exhibited high inhibitory activity with IC50＝0.82 g•mL－1.

Key words: thiohydrouracil, Hill reaction, inhibition, synthesis