| 天维菌素酰化衍生物的合成及杀虫杀螨活性 |
| |
| 引用本文： | 陈浩,张绍勇,韩群琦,张辉,王继栋,陈安良.天维菌素酰化衍生物的合成及杀虫杀螨活性[J].农药学学报,2020,22(1):35-47. |
| |
| 作者姓名： | 陈浩 张绍勇 韩群琦 张辉 王继栋 陈安良 |
| |
| 作者单位： | 浙江农林大学生物农药高效制备技术国家地方联合工程实验室,杭州 311300;湖州师范学院生命科学学院,浙江省媒介生物学与病原传播控制重点实验室,浙江湖州 313000;浙江省抗真菌药物重点实验室,浙江海正药业股份有限公司,浙江台州 318000 |
| |
| 基金项目： | 国家自然科学基金项目(31471809)；中国博士后科学基金(2018M630689) |
| |
| 摘 要： | 以天维菌素B、天维菌素B单糖苷和天维菌素B苷元为原料,经选择性C-5羟基保护,在C-13、C-4′和C-4″位引入不同酰基基团,合成了3个系列共23个天维菌素B酰化衍生物,并通过1H NMR、13C NMR和高分辨质谱对所有目标化合物的结构进行了表征。生物活性测定结果表明,所有衍生物对小菜蛾Plutella xylostella、朱砂叶螨Tetranychus cinnabarinus以及松材线虫Bursaphelenchus xylophilus均表现出不同程度的毒杀活性,其中天维菌素B C-4″位衍生物的活性优于C-4′位衍生物及13位衍生物。化合物8e对小菜蛾和松材线虫的毒杀活性最优,LC50值分别为9.2 mg/L和0.42 mg/L,化合物8b对朱砂叶螨的毒性最高,LC50值为0.0019 mg/L,均优于对照药天维菌素B。
|
| 关 键 词： | 天维菌素B 酰化衍生物 合成 杀虫活性 杀螨活性 |
| 收稿时间： | 2019-06-16 |
Synthesis,insecticidal and acaricidal activities of tenvermectin acylated derivatives |
| |
| CHEN Hao,ZHANG Shaoyong,HAN Qunqi,ZHANG Hui,WANG Jidong,CHEN Anliang.Synthesis,insecticidal and acaricidal activities of tenvermectin acylated derivatives[J].Chinese Journal of Pesticide Science,2020,22(1):35-47. |
| |
| Authors: | CHEN Hao ZHANG Shaoyong HAN Qunqi ZHANG Hui WANG Jidong CHEN Anliang |
| |
| Institution: | 1.Provincial Joint Engineering Laboratory of Biopesticide Preparation, Zhejiang A&F University, Hangzhou 311300, China2.Key Laboratory of Vector Biology and Pathogen Transmission Control in Zhejiang Province, College of Life Sciences, Huzhou University, Huzhou 313000, Zhejiang Province, China3.Zhejiang Key Laboratory of Antifungal Drugs, Zhejiang Hisun Pharmaceutical Co., Ltd, Taizhou 318000, Zhejiang Province, China |
| |
| Abstract: | Twenty-three derivatives of tenvermectin B, tenvermectin B monosaccharide and tenvermectin B aglycone were synthesized by introducing different acyl groups at the C-13, C-4′ and C-4′′ sites after the selective protection of C-5 hydroxyl group. All target compounds were characterized by 1H NMR, 13C NMR and high resolution mass spectra. Their insecticidal activities were tested against Plutella xylostella, Tetranychus cinnabarinus and Bursaphelenchus xylophilus. All the tested compounds showed significant secticidal activities against the above mentioned three insect species and the 4″-tenvermectin B derivatives were superior to the 4′- and 13-derivatives of tenvermectin B. Compound 8e displayed potentactivity to P. xylostella and B. xylophilus with LC50 values of 9.2 mg/L and 0.42 mg/L, respectively. Moreover, compound 8b showed the best inhibitory activity against T. cinnabarinus with LC50 value of 0.001 9 mg/L, which was superior to that of tenvermectin B. |
| |
| Keywords: | tenvermectin B acylaed derivatives synthesis insecticidal activity acaricidal activity |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
| 点击此处可从《农药学学报》浏览原始摘要信息 |
| 点击此处可从《农药学学报》下载免费的PDF全文 |
|
