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米尔贝霉素类似物的合成及杀螨杀蚜活性

Synthesis and insecticidal and acaricidal activities of milbemycins derivatives
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摘要 为寻找高活性的米尔贝霉素衍生物,以伊维菌素为原料,经脱糖、羟基保护、氧化、还原胺化、脱保护等将其转变为13-氨基米尔贝霉素类似物,通过三组分反应设计合成了一系列米尔贝霉素磺酰脒类化合物(7a~7i),并初步测定了其对朱砂叶螨Tetranychuscinnabarinus和豆蚜Aphiscraccivora的室内活性。结果表明:各衍生物对朱砂叶螨和豆蚜均有较好的触杀活性,其中7f、7h和7i对朱砂叶螨24h的LC50值分别为1.04×10-1、9.60×10-4和1.44×10-2mg/L;7i对豆蚜24h的LC,n值为7.81mg/L。米尔贝霉素13位氨基上磺酰化的结构修饰有助于提高米尔贝霉素类化合物的杀螨、杀蚜活性。 In order to find the high activity milbemycins derivatives. With ivermectin as the raw material, a series of 13-sulfonyl amidine-milbemycins derivatives (7a-7i) were synthesized after deglycosylation, hydroxy protection, oxidizing reaction, reductive amination and deprotection of C-13 of milbemycins. The preliminary bioassay showed that the compounds exhibited high insecticidal activity against Tetranychus cinnabarinus and Aphis craccivora. Some of them show a higher insecticidal activity, the LCs0 value of 7g, 7h and 7i against T. cinnabarinus were 1.04× 10-2, 9.60× 10-4, 1.44× 10-2 mg/L in 24 h, respectively, the LCs0 value of 7i against A. craccivora were 7.80 mg/L. The results indicate that the structural modification of sulfonylation on the C-13 amine of milbemycins are helpful to improve the activity against spide mite and aphid.
作者 余海涛 张健 胡冠芳 成丕乐 张娜 刘映前 YU Haitao1,2, ZHANG Jian3, HU Guanfang2, CHENG Peile3, ZHANG Na3, LIU Yingqian3 (1. Pratacultural College, Gansu Agricultral University, Lanzhou 730070, China; 2. Institute of Plant Protection, Gansu Academy of Agricultural Sciences, Lanzhou 730070, China; 3. Institute of Pharmaceutics Chemistry, School of Pharmaceutics, Lanzhou University, Lanzhou 730000, China)
出处 《农药学学报》 CSCD 北大核心 2017年第5期648-653,共6页 Chinese Journal of Pesticide Science
基金 国家地区科学基金项目(31760525).
关键词 米尔贝霉素类似物 合成 杀螨活性 杀蚜活性 milbemycins derivatives synthesis acaricidal activity insecticidal activity
作者简介 余海涛,男,博士研究生,主要从事植物源农药和农药环境毒理学研究,E-mail:yuhaita01202@163.com; 胡冠芳,共同通信作者,男,研究员,主要从事除草剂研究,E-mail:huguanfang@126.com 刘映前,通信作者,男,博士,教授,主要从事药物分子设计与合成和生物有机与药物化学研究,E-mail:yqliu@lzu.edu.cn
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