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2012 , Vol. 32 >Issue 07: 1278 - 1283

DOI: https://doi.org/10.6023/cjoc1111181

研究论文

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

  • 徐焱 ,
  • 王振 ,
  • 凌云 ,
  • 董玮 ,
  • 邢静 ,
  • 梁沛 ,
  • 杨新玲
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  • 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

收稿日期: 2011-11-18

  修回日期: 2011-12-17

  网络出版日期: 2012-03-22

基金资助

国家“十二五”科技支撑计划课题(No. 2011BAE06B05-5);国家973 计划(No. 2010CB126104)及国家高技术研究发展计划(“863”计划) (No. 2006AA10A201)资助项目.

收起

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

  • Xu Yan ,
  • Wang zhen ,
  • Ling Yun ,
  • Dong Wei ,
  • Xing Jing ,
  • Liang Pei ,
  • Yang Xinling
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  • 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

Received date: 2011-11-18

  Revised date: 2011-12-17

  Online published: 2012-03-22

Supported by

Project supported by the National Scientific and Technology Supporting Program of China (No. 2011BAE06B05-5), the National Key Project for Basic Research (No. 2010CB126104) and the National High Technology Research and Development Program (No. 2006AA10A201).

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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,本文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。

关键词： 苯丙醛; 缩氨基硫脲; 酪氨酸酶; 合成; 生物活性

本文引用格式

徐焱 , 王振 , 凌云 , 董玮 , 邢静 , 梁沛 , 杨新玲 . 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[J]. 有机化学, 2012 , 32(07) : 1278 -1283 . DOI: 10.6023/cjoc1111181

Abstract

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, 1H NMR, MS and EA. 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.

Key words： phenylpropyl aldehyde; thiosemicarbazone; tyrosinase; biological activity

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