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1-吡唑酰基-2-烷氧基羰基肼类化合物的合成及其生物活性

Synthesis of 1-Pyrazol-5′-ylcarbonyl-2-(alkyloxycarbonyl) hydrazides and Their Biological Activities

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【作者】 张广才; 雷树祥; 谭成侠;

【Author】 ZHANG Guang-cai~1,LEI Shu-xiang~(2a),TAN Cheng-xia~(2b)(1.Zhejiang Medicine Co.LTD.,Xinchang Pharmaceutical Factory, Xinchang 312500,China;a.Dean’s Office;b.College of Chemical Engineering and Material Science,2.Zhejiang University of Technology,Hangzhou 310014,China)

【机构】 浙江医药股份有限公司新昌制药厂; 浙江工业大学教务处; 浙江工业大学化学工程与材料学院 浙江新昌312500; 浙江杭州310014;

【摘要】 4-取代-1-甲基-3-乙基-5-吡唑甲酰肼与氯甲酸酯缩合得到16个1-吡唑酰基-2-烷氧基羰基肼类化合物(2a~2h和3a~3h,其中14个是新化合物),其结构经1H NMR,IR,MS和元素分析表征。初步生物活性测试结果表明,当浓度为500μg.mL-1时,3a,3b和3 e对油菜菌核病菌抑制活性均达到90%,3d对小麦白粉病菌的抑制活性达到90%;2h对蚕豆蚜的抑制活性达到92.75%。当浓度为1 000μg.mL-1时,2h对粘虫的抑制活性达到100%。

【Abstract】 1-Pyrazol-5′-ylcarbonyl-2-(alkyloxycarbonyl)hydrazides(2a2h and 3a3h,fourteen of them are novel compounds) were synthesized by a(condensation) reaction of 4-substituted-3-ethyl-1-methyl-5-pyrazole formhydrazide with chloroformate.Their structures were confirmed by 1H NMR,IR,MS and elemental analysis.The biological activity tests showed that 3a,3b and 3e exhibited excellent inhibitory activities(90%) against(sclerotinia) sclerotiorum,inhibitory activity of 3d was 90% against blumeria graminis,inhibitory activity of 2h was 92.75% against aphis fabae as 500 μg·mL-1;2h exhibited(excellent) inhibitory activity(100%) against mythimna separate as 1 000 μg·mL1.

【关键词】 吡唑; 酰肼; 生物活性; 合成;
【Key words】 pyrazole; hydrazide; biological activiy; synthesis;
【基金】 浙江省教育厅资助项目(20030145)
  • 【文献出处】 合成化学 ,Chinese Journal of Synthetic Chemistry , 编辑部邮箱 ,2006年05期
  • 【分类号】O626.21
  • 【被引频次】15
  • 【下载频次】306
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