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2012 , Vol. 32 >Issue 05: 957 - 961

DOI: https://doi.org/10.6023/cjoc1111162

研究简报

新型取代3-芳基-1,2,4-三唑并[3,4-b]苯并噻唑的合成及其杀菌活性

  • 翁建全 ,
  • 黄华 ,
  • 谭成侠 ,
  • 刘幸海 ,
  • 储为盛 ,
  • 陈杰
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  • a 浙江工业大学化学工程与材料学院 杭州 310032;
    b 国家南方农药创制中心浙江基地生测部 杭州 310023

收稿日期: 2011-10-16

  修回日期: 2011-12-13

  网络出版日期: 2012-01-06

基金资助

国家自然科学基金(No. 30900959)资助项目.

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Synthesis and Antifungal Activity of Novel Substituted- 3-aryl-1,2,4-triazolo[3,4-b]benzothiazoles

  • Weng Jianquan ,
  • Huang Hua ,
  • Tan Chengxia ,
  • Liu Xinghai ,
  • Chu Weisheng ,
  • Chen Jie
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  • a College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310032;
    b Bioassay Department, Zhejiang Branch of National Southern Pesticide Research Centre, Hangzhou 310023

Received date: 2011-10-16

  Revised date: 2011-12-13

  Online published: 2012-01-06

Supported by

Project supported by the National Natural Science Foundation of China (No. 30900959).

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摘要

为了寻找新的含苯并噻唑稠杂环农药先导化合物, 利用取代2-肼基苯并噻唑与取代苯甲酸在三氯氧磷中回流反应, 合成了18 个新型取代3-芳基-1,2,4-三唑并[3,4-b]苯并噻唑化合物, 并利用1H NMR, EI-MS 及元素分析对其结构进行了表征. 初步生物活性试验结果表明, 在50 mg/L 浓度下, 部分目标化合物对立枯丝核菌(Rhizoctonia solani)、西瓜壳二孢菌(Ascochyta citrullina)、香蕉枯萎病菌(Fusarium oxysporum f.sp. cubense)、烟草炭疽病菌(Colletotrichum nicotianae)具有中等杀菌活性. 然而, 部分化合物对灰葡萄孢菌(Botrytis cinerea)反而起到一定促进生长作用.

关键词： 1,2,4-三唑并[3,4-b]苯并噻唑; 合成; 杀菌活性

本文引用格式

翁建全 , 黄华 , 谭成侠 , 刘幸海 , 储为盛 , 陈杰 . 新型取代3-芳基-1,2,4-三唑并[3,4-b]苯并噻唑的合成及其杀菌活性[J]. 有机化学, 2012 , 32(05) : 957 -961 . DOI: 10.6023/cjoc1111162

Abstract

In order to find new benzothiazole lead compounds, eighteen new substitued-3-aryl-1,2,4-triazolo[3,4-b]-benzothiazoles were synthesized by reacting substituted-2-hydrazinobenzothiazole with various substituted benzoic acids in POCl3 under reflux condition. The structures of the title compounds were characterized by 1H NMR, EIMS techniques and elemental analysis. The preliminary bioassy results indicated that some of them showed moderate inhibition activity against Rhizoctonia solani, Ascochyta citrullina, Fusarium oxysporum f.sp. cubense and Colletotrichum nicotianae. Unexpectedly, some of them possessed certain promotion activity against Botrytis cinerea.

Key words： 1,2,4-triazolo[3,4-b]benzothiazole; synthesis; antifungal activity

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