取代苯丙醛缩氨基硫脲类化合物的合成及其对棉铃虫酪氨酸酶的生物活性研究  

Synthesis of Substituted Phenylpropyl Aldehyde Thiosemicarbazone Compounds and Their Bioactivity on Tyrosinase of Cotton Bollworm

作　　者：徐焱[1] 王振[1] 凌云[1] 董玮[2] 邢静[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》2012年第7期1278-1283,共6页Chinese Journal of Organic Chemistry

基　　金：国家"十二五"科技支撑计划课题(No.2011BAE06B05-5);国家973计划(No.2010CB126104);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,是一个潜在的农药作用靶标.为了发现新的农药先导化合物,在前期工作基础之上,设计了一系列取代苯丙醛缩氨基硫脲类化合物,以取代苯甲醛为起始原料,经5步反应合成了15个目标化合物,其结构通过红外、核磁氢谱、质谱及元素分析确认.生物活性测试结果表明,该系列化合物对棉铃虫酪氨酸酶活性均优于商品化药剂托酚酮.Tyrosinase played an important biological function in insect and might be a potent target for pest control. In order to find new lead of pesticide, a series of substituted phenylpropyl aldehyde thiosemicarbazone compounds were designed based on our previous work. The title compounds were synthesized from the starting material of substituted benzaldehyde in 5 steps. Their structures were characterized by IR, lH NMR, MS techniques and elemental analysis. The bioassay result showed that all of the title compounds exhibited higher inhibitory effect than commercial reagent tropolone on the tyrosinase of cotton bollworm, Helicoverpa armigera.

关 键 词：苯丙醛 缩氨基硫脲 酪氨酸酶 生物活性 

分 类 号：TQ450.21[化学工程—农药化工]