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  

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

作　　者：王振[1] 徐焱[1] 董玮[2] 梁沛[2] 杨新玲[1] 

机构地区：[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

出　　处：《有机化学》2011年第4期567-571,共5页Chinese Journal of Organic Chemistry

基　　金：国家高技术研究发展计划("863"计划)(No.2006AA10A201)资助项目

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、核磁氧谱、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.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 dia mondback moth Plutella xylostella （L.） were tested. The bioassay result showed that some of the title compounds exhibited inhibitory effect on the tyrosinase.

关 键 词：乙二酰胺 酪氨酸酶 合成 生物活性 

分 类 号：S482.3[农业科学—农药学]