米尔贝霉素类似物的合成及杀螨杀蚜活性 |
投稿时间:2017-04-23
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引用本文:余海涛,张健,胡冠芳,等.米尔贝霉素类似物的合成及杀螨杀蚜活性[J].农药学学报,2017,19(5):648-653. |
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基金项目:国家地区科学基金项目(31760525) |
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中文摘要: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Tetranychus cinnabarinus和豆蚜Aphis craccivora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24 h的LC50值分别为1.04×10–2、9.60×10–4和1.44×10–2 mg/L;7i对豆蚜24 h的LC50值为7.81 mg/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。 |
中文关键词:米尔贝霉素类似物 合成 杀螨活性 杀蚜活性 |
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Synthesis and insecticidal and acaricidal activities of milbemycins derivatives |
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Abstract: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 LC50 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 LC50 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. |
Key words:milbemycins derivatives synthesis acaricidal activity insecticidal activity |
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