含咪唑烷酮(吡咯甲酰胺)结构的三氟乙基硫醚(亚砜)类化合物的设计、合成及杀螨活性
Design,synthesis,and acaricidal activity of trifluoroethyl sulfide(sulfoxide)compounds containing imidazolidone(pyrrolamide)moieties
陈锦彪 1罗时燕 1田平义 2林健 2刘祈星 1周海峰1
作者信息
- 1. 三峡大学生物与制药学院天然产物研究与利用湖北省重点实验室绿色制药技术与工艺研究中心,湖北宜昌 443002
- 2. 顺毅股份有限公司台州市绿色农业化学品开发重点实验室,浙江台州 318000
- 折叠
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100mg/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.
Abstract
[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 Ⅸb and Xb had a mortality rate of over 96％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.
关键词
三氟乙基硫醚(亚砜)/咪唑烷酮衍生物/吡咯甲酰胺/杀螨活性/合成Key words
trifluoroethyl sulfide(sulfoxide)/imidazolidinone derivative/pyrrolamide/acaricidal activity/synthesis引用本文复制引用
基金项目
顺毅股份有限公司研发项目(SDHZ2021215)
国家自然科学基金(222278244)
出版年
2024
NETL
NSTL
万方数据