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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

Synthesis and Biological Activities of 1-Pyrazol-5′-yl carbonyl-2-substituted benzoylhydrazides

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【作者】 谭成侠沈德隆翁建全孙娜波欧晓明

【Author】 TAN Cheng-xia~(1*),SHEN De-long~1,WENG Jian-quan~1,SUN Na-bo~1,OU Xiao-ming~2 (1.College of Chemical Engineering and Materials Science,Zhejiang University of Technology,Hangzhou 310014,China;2.Bioassay Department,Hunan Branch of National Southern Pesticide Research Centre,Changsha 410007,China)

【机构】 浙江工业大学化学工程与材料学院国家南方农药创制中心湖南基地生测部 浙江杭州310032浙江杭州310032湖南长沙410007

【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,M S和元素分析确证。初步生物活性实验结果表明,在25μg/mL浓度下,3b和3 j对稻瘟病菌Pyricularia oryzae的抑制率分别为51.3%和56.1%;在1 000μg/mL下,3b对粘虫M ythimna separata的致死率达到100%。

【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.

【基金】 浙江省教育厅资助项目(20030145)
  • 【文献出处】 农药学学报 ,Chinese Journal of Pesticide Science , 编辑部邮箱 ,2006年04期
  • 【分类号】TQ450.26
  • 【被引频次】23
  • 【下载频次】502
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