4-芳基-3-羟基异噻唑衍生物的合成与生物活性研究  

Synthesis and Biological Activity of 4-Aryl-3-hydroxyisothiazole Derivatives

作　　者：周聪伟 林义峰 郭林朝 肖胜 巨修练 刘根炎 ZHOU Congwei;LIN Yifeng;GUO Linchao;XIAO Sheng;JU Xiulian;LIU Genyan(Key Laboratory for 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》2022年第4期24-28,共5页Chemistry & Bioengineering

基　　金：国家自然科学基金项目(22177090,21807082);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：以3-羟基异噻唑为原料,设计并合成了一系列4-芳基-3-羟基异噻唑衍生物,通过^(1)HNMR、^(13)CNMR和HRMS对目标化合物进行了结构表征,并测试了目标化合物的昆虫γ-氨基丁酸(GABA)受体抑制活性及杀虫活性。结果表明,目标化合物在100μmol·L^(-1)浓度下对斜纹夜蛾和家蝇GABA受体均具有一定的抑制活性,且部分目标化合物对斜纹夜蛾幼虫表现出一定的杀虫活性。Using 3-hydroxyisothiazole as a raw material,we designed and synthesized a series of 4-aryl-3-hydroxyisothiazole derivatives,and characterized the structures of the target compounds by ^(1)HNMR,^(13)CNMR,and HRMS.Moreover,we tested the insectγ-aminobutyric acid(GABA)receptor inhibitory activity and insecticidal activity of the target compounds.The results show that the target compounds have certain inhibitory activities against Spodoptera litura and Musca domestica GABA receptors at the concentration of 100μmol·L^(-1),and some of the target compounds show certain insecticidal activities against Spodoptera litura larvaes.

关 键 词：3-羟基异噻唑 GABA受体 竞争性拮抗剂 杀虫活性 

分 类 号：TQ453[化学工程—农药化工]