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鬼臼毒素4β含硫衍生物的 合成及其拒食活性
引用本文:陈利标,闫海燕,冯俊涛,李广泽,田瑄,张兴. 鬼臼毒素4β含硫衍生物的 合成及其拒食活性[J]. 农药学学报, 2006, 8(4): 359-362
作者姓名:陈利标  闫海燕  冯俊涛  李广泽  田瑄  张兴
作者单位:1.西北农林科技大学 无公害农药研究服务中心,陕西 杨凌 712100
基金项目:国家西部开发重大项目(2004BA901A14),西北农林科技大学科研专项
摘    要:为研究鬼臼毒素类化合物结构与杀虫活性的关系,在前期研究基础上设计合成了3个4β-硫酯-4-脱氧鬼臼毒素、2个4β-硫醚-4-脱氧鬼臼毒素及4β-巯基-4-脱氧鬼臼毒素共6个未见文献报道的化合物。其结构经IR、MS、1H NMR和元素分析确证。采用小叶碟添加法测试了化合物对3龄粘虫Mythimna separate幼虫的拒食活性,结果表明:4β-巯基-4-脱氧鬼臼毒素的活性最高,24和48 h 的AFC50(拒食中浓度)分别为164.6 和248.1 mg/L,分别是母体化合物鬼臼毒素活性的5.8和 3.0倍。引入硫醚及硫酯后活性均降低。

关 键 词:鬼臼毒素衍生物   4β-巯基-4-脱氧鬼臼毒素   合成   粘虫   拒食活性
文章编号:1008-7303(2006)04-0359-04
收稿时间:2006-07-18
修稿时间:2006-10-05

Synthesis and Antifeedant Activity of Podophyllotoxin Analogues with 4β Sulfur Substituted Groups
CHEN Li-biao,YAN Hai-yan,FENG Jun-tao,LI Guang-ze,TIAN Xuan and ZHANG Xing. Synthesis and Antifeedant Activity of Podophyllotoxin Analogues with 4β Sulfur Substituted Groups[J]. Chinese Journal of Pesticide Science, 2006, 8(4): 359-362
Authors:CHEN Li-biao  YAN Hai-yan  FENG Jun-tao  LI Guang-ze  TIAN Xuan  ZHANG Xing
Affiliation:1.Biorational Pesticide R& D Center of Northwest Sci-tech University of Agriculture and Forestry2.Shaanxi Research Center of Biopesticide Technology and Engineering,Yangling 712100,China3.Key State laboratory of Applied Organic Chemistry,Lanzhou University,Lanzhou 730000,China
Abstract:Three 4β-thioester-4-deoxypodophyllotoxins,two 4β-thioether-4-deoxypodophyllotoxins and one 4β-thiol-4-deoxypodophyllotoxin were synthesized,and their structures were confirmed by IR,MS,1H NMR and elemental analysis.The 24 h and 48 h antifeedant activities against the 3rd larvae of Mythimna separate were assayed with leaf-disk method.The bioassay results showed that 4β-thiol-4-deoxypodophyllotoxin had the highest activity among synthesized compounds.Its 24 h and 48 h AFC50(concentration for 50% antifeedant activity) were 164.6 and 248.1 mg/L,5.8 and 3.0 times of that of podophyllotoxin,respectively.4β-thioester and 4β-thioether derivatives had relative lower activities than the others.
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