Design, semisynthesis and insecticidal activity of novel podophyllotoxin derivatives against Brontispa longissima in vivo
Design, semisynthesis and insecticidal activity of novel podophyllotoxin derivatives against Brontispa longissima in vivo
复制标题
新型鬼臼毒素衍生物的设计、半合成及其体内杀虫活性
DOI：
10.1016/j.pestbp.2011.09.012
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发表时间：
2012-01-01
影响因子：
4.7
通讯作者：
Feng, Gang
中科院分区：
文献类型：
--
作者：
Liu, Ying-Qian;Zhao, Yong-Long;Feng, Gang
为了寻找有效的植物杀虫剂，首先合成了一系列新型鬼臼毒素衍生物，并初步测试了其对长叶椰心甲五龄幼虫的拒食和杀虫作用。化合物3a-1的不同拒食和杀虫活性范围表明鬼臼毒素骨架4位NR(1)R(2)基团的变化显着影响了该类化合物的活性谱，并从中揭示了一些重要的SAR信息。为了阐明其杀虫活性的作用方式，还研究了代表性化合物3i的时钟模型以及微管蛋白抑制作用，结果表明这些化合物的杀虫活性是由于这些衍生物的微管蛋白抑制作用，从而可能为新型鬼臼毒素类杀虫剂的合理设计提供一些有用的信息。 (C) 2011 Elsevier Inc. 保留所有权利。
In an attempt to find the effective phytopesticides, a series of novel podophyllotoxin derivatives were firstly synthesized and preliminarily tested for their antifeedant and insecticidal effects against the fifth-instar larvae of Brontispa longissima. The different antifeedant and insecticidal activity ranges of compounds 3a-1 showed that variations of NR(1)R(2) groups in the 4-position of podophyllotoxin skeleton markedly affected the activity profiles of this compound class, and some important SAR information has been revealed from it. To clarify their mode of action of insecticidal activity, the clocking models as well as tubulin inhibitory effect of representative compound 3i were also investigated, and the result indicated that the insecticidal activity of these compounds was due to the tubulin inhibitory effect of these derivatives, thereby possibly providing some useful information for rational designs of novel podophyllotoxin-based insecticides. (C) 2011 Elsevier Inc. All rights reserved.