含氟吡唑-4-肟酯乙酰胺类衍生物的合成及生物活性

Synthesis and biological activity of fluorinated 1H-pyrazole-4-oxime ester-acetamides derivatives

摘要: 为寻求具有较高生物活性的农药新品种，以杀螨剂pyflubumide为先导，在其母体结构中引入肟酯和二芳基醚结构，设计并合成了7个未见文献报道的1H-吡唑-4-肟酯乙酰胺类化合物，其结构均经核磁共振氢谱、质谱和元素分析确证。初步生物活性测试结果表明，在500 mg/L 质量浓度下，所有目标化合物对朱砂叶螨Tetranychus cinnabarinus 均有较强的杀灭作用，大部分化合物对其的致死率达100%，但药效低于对照药剂阿维菌素和炔螨特。

Abstract: To find new biological lead compounds with high bioactivity, 7 new 1H-pyrazole-4-oxime ester-acetamides derivatives were designed and synthesized by inserting the oxime esters and tolyloxybenzyl into mother structure of pyflubumide. Their structures were confirmed by 1H NMR, MS and elemental analysis. The acaricidal activity of these compounds was evaluated. The results showed that most of title compounds exhibited inhibiting effect against Tetranychus cinnabarinus with 100% death rate at 500 mg/L. However,the effect is not as well as abamectin or propargite.