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1-吡唑甲酰基-2-芳基酰肼类化合物的合成及生物活性
引用本文:谭成侠,沈德隆,翁建全,孙娜波,欧晓明.1-吡唑甲酰基-2-芳基酰肼类化合物的合成及生物活性[J].农药学学报,2006,8(4):363-366.
作者姓名:谭成侠  沈德隆  翁建全  孙娜波  欧晓明
作者单位:1.浙江工业大学 化学工程与材料学院,浙江 杭州 310032
基金项目:浙江省教育厅资助项目(20030145)
摘    要:为了寻求新的含吡唑双酰肼类先导化合物,用4-取代-1-甲基-3-乙基-5-吡唑甲酰肼与取代苯甲(乙)酰氯进行缩合反应得到了10个1-吡唑甲酰基-2-芳基酰肼类化合物,其中9个是新化合物,其结构经IR,1H NMR,MS和元素分析确证。初步生物活性实验结果表明,在25 μg/mL浓度下, 3b 和 3j 对稻瘟病菌Pyricularia oryzae的抑制率分别为51.3%和56.1%;在1 000 μg/mL下, 3b 对粘虫Mythimna separata的致死率达到100%。

关 键 词:1-吡唑甲酰基-2-芳基酰肼类化合物    合成    生物活性
文章编号:1008-7303(2006)04-0363-04
收稿时间:08 3 2006 12:00AM
修稿时间:10 30 2006 12:00AM

Synthesis and Biological Activities of 1-Pyrazol-5'-yl carbonyl -2-substituted benzoylhydrazides
TAN Cheng-xi,SHEN De-long,WENG Jian-quan,SUN Na-bo and OU Xiao-ming.Synthesis and Biological Activities of 1-Pyrazol-5''-yl carbonyl -2-substituted benzoylhydrazides[J].Chinese Journal of Pesticide Science,2006,8(4):363-366.
Authors:TAN Cheng-xi  SHEN De-long  WENG Jian-quan  SUN Na-bo and OU Xiao-ming
Institution:1.College of Chemical Engineering and Materials Science,Zhejiang University of Technology,Hangzhou 310014, China2.Bioassay Department,Hunan Branch of National Southern Pesticide Research Centre,Changsha 410007,China
Abstract:In order to find new lead compounds,9 novel and one known 1-pyrazol-5'-yl carbonyl-2-substituted benzoylhydrazides were prepared by a condensation reaction of 4-substituted -3-ethyl-1-methyl-5-pyrazole formhydrazide and substituted benzoyl chloride,and their structures were confirmed by 1H NMR,MS,IR and elemental analysis.The preliminary bioassay showed that compounds 3b and 3j exhibited 51.3% and 56.1% inhibition rate against Pyricularia oryzae at 500 μg/mL,respectively. 3b showed excellent fatality rate (100%) against Mythimna separate at 1 000 μg/mL.
Keywords:1-pyrazol-5'-yl carbonyl-2-substituted benzoylhydrazides  synthesis  biological activities
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