含肟醚片段的二苯醚脒类化合物的设计、合成及生物活性  

Design, synthesis and biological activity of diphenyletheramidinecompounds containing oxime ethers moiety

作　　者：严康 李宏伟 曹晓峰 王金娥 吕亮 邵旭升[1] YAN Kang;LI Hongwei;CAO Xiaofeng;WANG Jin'e;LYU Liang;SHAO Xusheng(East China University of Science and Techology,Shanghai 200000,China;CAC Nantong Chemicals Co.,Ltd.,Nantong 226407,Jiangsu,China;Shanghai Greentech Laboratory Co.,Ltd.,Shanghai 201612,China)

机构地区：[1]华东理工大学药学院,上海200000 [2]南通泰禾化工股份有限公司,江苏南通226407 [3]上海晓明检测技术有限公司,上海201612

出　　处：《农药》2023年第11期795-799,共5页Agrochemicals

基　　金：国家自然科学基金(编号:21877039和32072441);上海市教委创新计划(2017-01-07-00-02-E00037);上海细胞代谢光遗传学技术前沿科学研究基地(上海市教委员会,2021科技03-28)

摘　　要：[目的]寻找具有高杀菌活性的农药先导化合物。[方法]通过活性亚结构拼接法设计并合成一系列的含肟醚片段的二苯醚脒类化合物,其结构经过1H NMR和LCMS确证。[结果]杀菌活性测试结果表明:目标化合物对黄瓜白粉病(Erysiphe cichoracearum)、大豆锈病(Phakopsora pachyrhizi)以及黄瓜霜霉病(Pseudoperonospora cubensis)具有一定的防治效果。其中化合物1b在40 mg/L质量浓度下对黄瓜白粉病的防治效果为100.00%;1a、1b在质量浓度为40 mg/L下对大豆锈病的防治效果均为92.59%;1f在100 mg/L质量浓度下对黄瓜霜霉病的防治效果为100.00%。[结论]含肟醚片段的二苯醚脒类化合物具有一定的杀菌活性,值得进一步研究。[Aims]This study aims to generate lead compound of fungicide with high fungicidal activities.[Methods]A series of diphenyletheramidine compounds containing oxime ethers moiety were designed by active substructure splicing method and synthesized.The structures of synthesized compounds were identified by 1H NMR and LCMS.[Results]The fungicidal activities results indicated that the target compounds exhibited certain control effects on Erysiphe cichoracearum,Phakopsora pachyrhizi and Pseudoperonospora cubensis.The control efficacy of compound 1b at 40 mg/L against E.cichoracearum was 100.00%,and the control efficacy of 1a and 1b at 40 mg/L against P.pachyrhizi was 92.59%.The control efficacy of 1f against P.cubensis at concentration of 100 mg/L was 100.00%.[Conclusions]Diphenyletheramidine compounds containing oxime ethers moiety have certain fungicidal activities and are worthy of further research.

关 键 词：合成 肟醚 二苯醚脒类化合物 杀菌活性 

分 类 号：TQ455.4[化学工程—农药化工]