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有机化学.pdfVIP

2011 年第 31 卷 有 机 化 学 Vol. 31, 2011 第 4 期, 567～571 Chinese Journal of Organic Chemistry No. 4, 567～571 ·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 a a b b *,a 王 振 徐 焱 董 玮 梁 沛 杨新玲 (a 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) (b 中国农业大学农学与生物技术学院 北京 100193) 摘要 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 Synthesis of Oxalamide Compounds Containing Pyrimidine and Their Bioactivity on Tyrosinase of Diamondback Moth Plutella xylostella (L.) Wang, Zhena Xu, Yana Dong, Weib Liang, Peib Yang, Xinling*,a a ( Key Laboratory of Pesticide Chemistry and Application, Ministry of Agriculture, College of Science, China Agricultural University, Beijing 100193) (b College of Agriculture and Biotechnology, China Agricultural University, Beijing 100193) Abstract Tyrosinase is an important enzyme in insect. The development of insect can be affected by regu- lating its tyrosinase activity. In this paper, ten new oxalamide compouds containing pyrimidine were de- signed 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