4,5-双取代-3-羟基异噻唑衍生物的合成与杀虫活性研究  

Synthesis and Insecticidal Activity of 4,5-Disubstituted-3-hydroxyisothiazole Derivatives

作　　者：熊壮 谢程 郭顺 刘根炎 XIONG Zhuang;XIE Cheng;GUO Shun;LIU Genyan(Key Laboratory of Green Chemical Process of Ministry of Education,Hubei Key Laboratory of Novel Reactor and Green Chemical Technology,School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430205,China)

机构地区：[1]武汉工程大学化工与制药学院、绿色化工过程教育部重点实验室、新型反应器与绿色化学工艺湖北省重点实验室,湖北武汉430205

出　　处：《化学与生物工程》2023年第5期25-29,37,共6页Chemistry & Bioengineering

基　　金：国家自然科学基金项目(22177090,21807082);湖北省教育厅科学技术研究项目(D20221503);湖北省高等学校优秀中青年科技创新团队计划项目(T201908);湖北省中央引导地方科技发展专项资金项目(2020ZYYD040)。

摘　　要：针对离子型γ-氨基丁酸(GABA)受体竞争性拮抗位点,设计合成了一系列5-芳基-4-四氢吡啶-3-羟基异噻唑衍生物,通过1HNMR、13CNMR和MS对目标化合物进行了结构表征。活性测试结果表明,在100 mg·L^(-1)浓度下,部分目标化合物对成年雌性果蝇表现出一定的杀虫活性,为新型GABA受体杀虫剂先导化合物的设计与合成提供了理论依据。We designed and synthesized a series of 5-aryl-4-tetrahydropyridine-3-hydroxyisothiazole derivatives on the basis of the competitive antagonistic sites of ionotropicγ-aminobutyric acid(GABA)receptors.Moreover,we characterized the structures of the target compounds by 1 HNMR,13 CNMR,and MS.The activity experiment results indicate that some of the target compounds show certain insecticidal activity against Drosophila melanogaster at the concentration of 100 mg·L^(-1).The study provides a theoretical basis and reference for the design and synthesis of novel insecticide leads of GABA receptors.

关 键 词：GABA受体 3-羟基异噻唑 竞争性拮抗剂 杀虫活性 

分 类 号：TQ453.2[化学工程—农药化工]