首页|新型1,2,3-噻二唑类化合物的设计、合成及生物活性

新型1,2,3-噻二唑类化合物的设计、合成及生物活性

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[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.
Design,synthesis and insecticidal activity of novel 1,2,3-thiadiazoles
[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 1H 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 1a,1b,1d,1e and 1h against P.xylostella and M.separata were all greater than 90%at 100 mg/L,the mortality rates of compounds 1a and 1e against T.cinnabarinus were greater than 90%at 100 mg/L,and the morta1ity rates of compounds 1a and 1e 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.

synthesis1,2,3-thiadiazoleinsecticidal activity

韩春波、张嘉博、曹晓峰、王文术、程家高、吕亮

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华东理工大学药学院,上海 200237

南通泰禾化工股份有限公司,江苏南通 226407

上海晓明检测技术有限公司,上海 201612

合成 1,2,3-噻二唑 杀虫活性

2024

农药
沈阳化工研究院有限公司

农药

CSTPCD北大核心
影响因子:0.665
ISSN:1006-0413
年,卷(期):2024.63(2)
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