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新型1,2,3-噻二唑类化合物的设计、合成及生物活性

Design,synthesis and insecticidal activity of novel 1,2,3-thiadiazoles
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摘要 [目的]为寻找高活性的农药先导化合物。[方法]通过活性亚结构拼接设计并合成了一系列1,2,3-噻二唑类化合物,所有结构经过1H NMR和LC-MS确证。[结果]大部分化合物对小菜蛾、黏虫、朱砂叶螨和褐飞虱表现出一定的杀虫活性。其中,化合物1a、1b、1d、1e和1h在100 mg/L质量浓度下对小菜蛾、黏虫的致死率均在90%以上,化合物1a和1e在100 mg/L质量浓度下对朱砂叶螨的致死率均在90%以上,化合物1a和1e在400 mg/L质量浓度下对褐飞虱的致死率均在90%以上。[结论]设计的1,2,3-噻二唑类化合物具有一定的杀虫活性,结构新颖,具有进一步研究价值。 [Aims]This study aims to find lead compounds with high activity.[Methods]A series of 1,2,3-thiadiazole compounds were designed by active substructure splicing method and synthesized.The structures of the target compounds were identified by'H NMR and LC-MS.[Results]Most of the compounds exhibited good insecticidal activity against Plutella xylostella,Mythimna separata,Tetranychus cinnabarinus and Nilaparvata lugens.The mortality rates of compounds la,Ib,1d,le and 1h against P.xylostella and M.separata were all greater than 90%at 100 mg/L,the mortality rates of compounds la and 1e against T.cinnabarinus were greater than 90%at 100 mg/L,and the mortality rates of compounds la and le against N.lugens were greater than 90%at 400 mg/L.[Conclusions]This series of 1,2,3-thiadiazole compounds have certain insecticidal activities,novel structures and value for further research.
作者 韩春波 张嘉博 曹晓峰 王文术 程家高 吕亮 HAN Chunbo;ZHANG Jiabo;CAO Xiaofeng;WANG Wenshu;CHENG Jiagao;LYU Liang(School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China;CAC Nantong Chemicals Co.,Ltd.,Nantong 226407,Jiangsu,China;Shanghai Greentech Laboratory Co.,Ltd.,Shanghai 201612,China)
出处 《农药》 CAS CSCD 北大核心 2024年第2期84-88,共5页 Agrochemicals
关键词 合成 1 2 3-噻二唑 杀虫活性 synthesis 1,2,3-thiadiazole insecticidal activity
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