新型含酰基脲桥和硫脲桥的苯双酰胺类似物的合成及生物活性

Synthesis and Biological Activities of Novel Analogues of Phthalamide Containing Acylurea and Acylthiourea

参考氟虫酰胺和除虫脲的活性结构片段,设计合成了一系列结构新颖的含有酰基脲桥和酰基硫脲桥的化合物,通过核磁共振氢谱、高分辨质谱以及X射线单晶衍射确定了其结构.生测结果表明,酰基脲桥和酰基硫脲桥结构的引入使杀虫活性降低,但是化合物7d在10 mg/L的浓度下,仍表现出一定的杀粘虫活性.此外发现部分化合物具有一定的抑菌活性,其中化合物8f对苹果轮纹、小麦纹枯和水稻恶苗病原菌的抑制率分别为75.0%、87.5%和84.6%.

In order to find novel and efficient insecticides targeting at the ryanodine receptor, a series of novel compounds containing acylurea and acylthiourea, referring to moieties of flubendiamide and diflubenzuron, were designed and synthesized. Their structures were characterized by 1H NMR, HRMS and X-ray diffraction. The insectical activities showed that the introducing of acylurea and acylthiourea bridges decreased the acitivity. Compound 7d showed 50% activity at the concentration of 10 mg/L. In addtion, some structures showed moderate antifungal activities. Compound 8f displayed 75.0%, 87.5% and 84.6% antifungal activities against Botryosphaeria dothidea, Rhizoctonia cerealis and Fusarium fujikuroi.