摘要
[目的]研发高活性三氟乙基硫醚(亚砜)类杀螨剂。[方法]以2-氟-4-甲基-5-((2,2,2-三氟乙基)硫基)苯胺为核心骨架,设计合成了系列含咪唑烷酮/吡咯甲酰胺结构的三氟乙基硫醚(亚砜)类新化合物,并对其进行了杀螨活性测试。[结果]在质量浓度为100 mg/L时,目标化合物具有一定的杀螨活性,其中化合物Ⅸb和Ⅹb对朱砂叶螨卵的致死率在96%以上,化合物Ⅸa对二斑叶螨成虫的致死率为100%。[结论]目标化合物具有较好的杀螨活性,为三氟乙基硫醚(亚砜)衍生物的设计和改造提供研究思路,对探究该类化合物的生物活性多样性具有参考意义。
[Aims] This study aims to generate trifluoroethyl sulfide(sulfoxide) compounds with excellent acaricidal activity. [Methods] A series of novel trifluoroethyl sulfide(sulfoxide) compounds containing imidazolidone(pyrrolamide) moieties were designed and synthesized from 2-fluoro-4-methyl-5-(2, 2, 2-trifluoroethylthio)aniline,and their acaricidal activity were tested. [Results] The activity results indicated that the synthesized compounds had certain acaricidal activity at the dosage of 100 mg/L. Compounds Ⅸ b and Ⅹ b had a mortality rate of over96% against the egg of Tetranychus cinnabarinus, and compound Ⅸa has a mortality rate of 100% against the T. urticae adults. [Conclusions] The target compounds with good acaricidal activity provide a guideline for the design of trifluoroethyl sulfide(sulfoxide) compounds and are of significant reference for exploring the biological activities diversity.
作者
陈锦彪
罗时燕
田平义
林健
刘祈星
周海峰
CHEN Jinbiao;LUO Shiyan;TIAN Pingyi;LIN Jian;LIU Qixing;ZHOU Haifeng(Research Center of Green Pharmaceutical Technology and Process,Hubei Key Laboratory of Natural Products Research and Development,College of Biological and Pharmaceutical Sciences,China Three Gorges University,Yichang 443002,Hubei,China;Taizhou Key Laboratory of Green Agrochemicals Development,Synwill Co.,Ltd.,Taizhou 318000,Zhejiang,China)
出处
《农药》
CAS
CSCD
北大核心
2024年第3期168-173,180,共7页
Agrochemicals
基金
顺毅股份有限公司研发项目(SDHZ2021215)
国家自然科学基金(222278244)。
作者简介
陈锦彪(1999-),男,湖北宜昌人,硕士,主要从事新农药创制研究。E-mail:1274878493@qq.com。;通信作者:刘祈星(1986-),男,江西安义人,博士,副教授,主要从事新农药创制、药物化学、有机化学研究。E-mail:qixingliu86@163.com。;通信作者:周海峰(1979-),男,湖北宜昌人,博士,教授,主要从事有机合成研究。E-mail:zhouhf@ctgu.edu.cn。
