摘要/Abstract

根据活性亚结构拼接原理，以阿维菌素B1a为先导化合物，经过酰胺化和点击反应合成了一系列含酰胺结构的4"-阿维菌素三唑类衍生物，并通过¹H NMR、¹³C NMR和高分辨质谱对目标化合物进行结构表征.初步的生物活性测定结果表明，目标化合物对朱砂叶螨、桃蚜和秀丽隐杆线虫均具有一定的杀虫活性.在0.1μg/mL浓度下，4"-（1-（4-（2-（4-氯苯基）-3-甲基丁酰胺基）-1H-1，2，3-三唑基）乙酰胺基）阿维菌素B1a（11b）和4"-（1-（4-氯苯甲酰胺基）-1H-1，2，3-三唑基）乙酰胺基）阿维菌素B1a（11e）对朱砂叶螨的杀虫活性达到83.5%和81.2%；4"-（1-（2-氨基-3-甲基苯乙酰胺基）-1H-1，2，3-三唑基）乙酰胺基）阿维菌素B1a（11i）对桃蚜（c：50 μg/mL）和秀丽隐杆线虫（1 μg/mL）的杀虫活性分别为86.4%和74.6%，优于对照药阿维菌素B1a.
关键词: 酰胺, 1,2,3-三唑, 阿维菌素B1a, 杀虫活性
Based on avermectin structure framework, a series of novel 4"-avermectin triazole derivatives containing amide unit were synthesized via the method of click reaction and amidation. The structures of target compounds were fully characterized by ¹H NMR, ¹³C NMR and HRMS. The preliminary bioassay showed that the target compounds possessed certain insceticidal activities against Tetranychus cinnabarinus, Myzus persicae and Caenorhabditis elegans. At the concentration of 0.1 μg/mL, the lethal rates of 4"-(1-(4-(2-(4-chlorphenyl)-3-methylbutylamido)-1H-1, 2, 3-triazolyl)acetamido)avermectin B1a (11b) and 4"-(1-(4-chlorobenzoamido)-1H-1, 2, 3-triazolyl)acetamido)avermectin B1a (11e) against Tetranychus cinnabarinus were 83.5% and 81.2%, respectively, and the lethal rates of 4"-(1-(2-amido-3-methylphenylethylamido)-1H-1, 2, 3- triazolyl)acetamido)avermectin B1a (11i) against Myzus persicae (c=50 μg/mL) and Caenorhabditis elegans (c=1 μg/mL) were 86.4% and 74.6%, which were better than that of avermetcin B1a.
Key words: amide, 1, 2, 3-triazole, avermectin B1a, insecticidal activity


PDF全文下载地址:

点我下载PDF