新型1H-吡唑-5-甲酰基氨基脲类化合物的合成及生物活性

采用活性亚结构拼接和生物合理设计的方法,将4-氯-1-甲基-3-乙基-5-吡唑甲酰肼与取代苯基异氰酸酯反应得到14个新的含氨基脲的吡唑类化合物。其结构经IR、1H NMR、质谱和元素分析确证。初步生物活性实验结果表明, 化合物1-( 4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基) -4-(2-甲基苯基)氨基脲( 4g) , 1-( 4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基) -4-( 4-氯苯基)氨基脲( 4b)在500μg /mL 剂量下对小麦白粉病菌Bumeria graminis和粘虫Mythimna separata 的抑制率和致死率分别达到90%和100%。

Synthesis and Biological Activities of Novel 1H-Pyrazole-5-formylsemi carbazide

In order to find new semicarbazide lead compounds, fourteen 4-phenyl-1-pyrazoleformylsem i- bazide were synthesized from 4-chloro-3-ethyl-1-methyl-5-pyrazole form hydrazide and substituted phenylisocyanate. The structures of all new compounds were confirmed by 1 H NMR, IR, MS and elementary analysis. The results of biological tests indicated that 1-( 4-chloro-3-ethy l-1-methyl-1H-pyrazole-5-formyl) -4-(2-methyl-phenyl) semicarbazide ( 4g ) and 1-( 4-chloro-3-ethy l-1-methyl-1H- pyrazole-5-formyl) -4-( 4-chloro-phenyl) semicarbazide ( 4b) showed 90% inhibition rate under the concentration of 500μg /mL against Blumeria graminis and 100% mortality rate to Mythimna separata, respectively.