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

作　　者：陈有为[1] 万莹莹[1] 刘巧霞[1] 刘敬波[1] 熊丽霞[1] 于淑晶[1] 李正名[1] 

机构地区：[1]南开大学元素有机化学研究所,元素有机化学国家重点实验室,天津化学化工协同创新中心,天津300071

出　　处：《有机化学》2015年第4期882-889,共8页Chinese Journal of Organic Chemistry

基　　金：国家重点基础研究发展计划(973计划,No.2010CB126106);国家自然科学基金(Nos.31370039,21272129);国家科技攻关计划(No.2011BAE06B05);高等学校博士学科点专项科研基金(No.20110031110017)资助项目~~

摘　　要：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.

关 键 词：氟虫酰胺 除虫脲 酰基脲桥 硫脲桥 杀虫活性 抑菌活性 

分 类 号：O625.6[理学—有机化学]