新型1H-吡唑-5-甲酰基氨基脲类化合物的合成及生物活性

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

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B lumeria gram inis和粘虫M ythimna separata的抑制率和致死率分别达到90%和100%。

In order to find new semicarbazide lead compounds, fourteen 4-phenyl-l-pyrazoleformylsemi- bazide were synthesized from 4-chloro-3-ethyl-l-methyl-5-pyrazole formhydrazide and substituted phenylisocyanate. The structures of all new compounds were confirmed by 1H NMR, IR, MS and elementary analysis. The results of biological tests indicated that 1-（ 4-chloro-3-ethyl-l-methyl-lH- pyrazole-5-formyl） -4- （ 2-methyl-phenyl ） semicarbazide （ 4g ） and 1- （ 4-chloro-3-ethyl-l-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.