含氟吡唑-4-肟酯乙酰胺类衍生物的合成及生物活性

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。

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

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.