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含N-吡啶联吡唑杂环的(磺)酰胺类化合物的设计、合成及生物活性
引用本文:徐俊英,董卫莉,熊丽霞,李正名.含N-吡啶联吡唑杂环的(磺)酰胺类化合物的设计、合成及生物活性[J].高等学校化学学报,2012,33(2):298-302.
作者姓名:徐俊英  董卫莉  熊丽霞  李正名
作者单位:1. 中国海洋石油总公司天津化工研究设计院, 工业节水国家重点实验室, 天津 300131; 2. 天津医科大学药学院, 天津 300070; 3. 南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 农药国家工程中心, 天津 300071
基金项目:国家"九七三"计划项目,国家自然科学基金
摘    要:以氯虫酰胺结构为基础, 设计合成了一系列含N-吡啶联吡唑杂环的酰胺及磺酰胺类化合物. 所有化合物的结构均通过元素分析和 1H NMR确证. 生物活性测试结果表明, 部分化合物对东方粘虫(4龄幼虫)和尖音库蚊(幼虫)表现出较好的杀灭活性. 化合物4a, 4k和5b在浓度为100 mg/L时对东方粘虫(4龄幼虫)的致死率均高于50%, 化合物4g 在浓度为2 mg/L时对尖音库蚊(幼虫)的致死率达100%.

关 键 词:氯虫酰胺  酰胺  磺酰胺  生物活性  
收稿时间:2011-02-25

Design, Synthesis and Biological Activities of Amides(Sulfonamides)Containing N-Pyridylpyrazole
XU Jun-Ying , DONG Wei-Li , XIONG Li-Xia , LI Zheng-Ming.Design, Synthesis and Biological Activities of Amides(Sulfonamides)Containing N-Pyridylpyrazole[J].Chemical Research In Chinese Universities,2012,33(2):298-302.
Authors:XU Jun-Ying  DONG Wei-Li  XIONG Li-Xia  LI Zheng-Ming
Institution:1. State-key Laboratory of Industrial Water-saving and Waste Water Reuse, Tianjin Chemical Research & Design Institute, China National Offshore Oil Corporation, Tianjin 300131, China; 2. College of Pharmacy, Tianjin Medical University, Tianjin 300070, China; 3. State Key Laboratory of Elemento-organic Chemistry, National Pesticide Engineering Research Center, Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071, China
Abstract:Referring to the structure of RynaxypyrTM,a series of novel amides(sulfonamides) containing N-pyridylpyrazole was designed and synthesized.Their chemical structures were characterized by means of 1H NMR and elemental analysis.The results of the biological assay show that some of the amide(subfonamides) exhibite good insecticidal activities against Oriental Armyworm(Mythimna separata Walker) and Culex pipiens pallens.The death rates for Oriental Armyworm of compounds 4a,4k and 5b are all higher than 50% at 100 mg/L,and the death rate of compound 4g for Culex pipiens pallens was 100% at 2 mg/L.
Keywords:RynaxypyrTM  Amide  Sulfonamide  Biological activity
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