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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (04): 567-571. 上一篇    下一篇

研究简报

含嘧啶环乙二酰胺类化合物的合成及其对小菜蛾酪氨酸酶的抑制作用

王振1，徐焱1，董玮2，梁沛2，杨新玲*,1   

  1. (1中国农业大学理学院 农业部农药化学与应用重点开放实验室 北京 100193)
    (2中国农业大学农学与生物技术学院 北京 100193)
  • 收稿日期:2010-03-22 修回日期:2010-11-15 发布日期:2010-12-03
  • 通讯作者: 王振 E-mail:wz1022@163.com
  • 基金资助:

    863计划项目

Synthesis of Oxalamide Compounds Containing Pyrimidine and Their Bioactivity on Tyrosinase of Diamondback Moth Plutella xylostella (L.)

Wang Zhen1 Xu Yan1 Dong Wei2 Liang Pei2 Yang Xinling*,1   

  1. (1 Key Laboratory of Pesticide Chemistry and Application, Ministry of Agriculture, College of Science, China Agricultural University, Beijing 100193)
    (2 College of Agriculture and Biotechnology, China Agricultural University, Beijing 100193)
  • Received:2010-03-22 Revised:2010-11-15 Published:2010-12-03

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1371

被引次数

16 | 4

酪氨酸酶在昆虫体内起着很重要的生理作用, 控制酪氨酸酶的活性即可调节昆虫的生长行为, 借鉴曲酸和铜铁试剂的杂原子螯合机理, 设计了一类含嘧啶环乙二酰胺的新型化合物, 以取代苯胺为起始原料经3步反应合成了目标化合物, 其结构通过红外、核磁氢谱、质谱、高分辨质谱表征. 生物活性测试表明该系列化合物对小菜蛾酪氨酸酶活性有一定的抑制作用.

关键词: 乙二酰胺, 酪氨酸酶, 合成, 生物活性

Tyrosinase is an important enzyme in insect. The development of insect can be affected by regulating its tyrosinase activity. In this paper, ten new oxalamide compouds containing pyrimidine were designed based on the mechanism of heteroatom chelation with kojic acid and cupferron. The title compounds were synthesized from the starting material of substituted aniline in 3 steps. Their structures were characterized by IR, 1H NMR, MS and HRMS techniques. Meanwhile, their effects on the tyrosinase of the diamondback moth Plutella xylostella (L.) were tested. The bioassay result showed that some of the title compounds exhibited inhibitory effect on the tyrosinase.

Key words: oxalamide, tyrosinase, synthesis, biological activity