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

作　　者：谭成侠[1] 沈德隆[1] 翁建全[1] 孙娜波[1] 欧晓明 

机构地区：[1]浙江工业大学化学工程与材料学院,浙江杭州310032 [2]国家南方农药创制中心湖南基地生测部,湖南长沙410007

出　　处：《农药学学报》2006年第4期363-366,共4页Chinese Journal of Pesticide Science

基　　金：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,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%。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.

关 键 词：1-吡唑甲酰基-2-芳基酰肼类化合物 合成 生物活性 

分 类 号：O626.21[理学—有机化学]