SYNTHESIS OF 2′(2′,6′)-(DI)HALOGENOISOXAZOLOPODOPHYLLIC ACIDS-BASED AMIDES DERIVED FROM A NATURALLY OCCURRING LIGNAN PODOPHYLLOTOXIN AND THEIR ACARICIDAL ACTIVITY

被引：3

作者：

Zhang, Bingchuan

Yu, Mingqiao

Lv, Min ^{[1
]}

Xu, Hui ^{[1
]}

机构：

[1] Northwest A&F Univ, Coll Plant Protect Chem & Pharm, Res Inst Pesticidal Design & Synth, Yangling 712100, Shaanxi, Peoples R China

来源：

HETEROCYCLES | 2018年 / 97卷 / 01期

基金：

中国国家自然科学基金;

关键词：

BIOLOGICAL-ACTIVITIES; OXIME DERIVATIVES; BIOSYNTHESIS; INSIGHT; MODE; QSAR;

D O I：

10.3987/COM-17-S(T)12

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In continuation of our program to discover natural product-based pesticides, a series of 2'(2',6)-(di)halogenoisoxazolopodophyllic acids-based amides were prepared by structural modification of a naturally occurring lignan podophyllotoxin. Meanwhile, their acaricidal activity was evaluated against a typically crop-threatening agricultural insect pest, Tetranychus cinnabarinus. Among all derivatives, especially compounds 10-12 displayed 4.8-7.4 folds more potent acaricidal activity than podophyllotoxin against T. cinnabarinus. This demonstrated that the carboxyl group at their C-2 position of 2'(2',6')-(di)halogenoisoxazolopodophyllic acids was very important for the acaricidal activity.

引用

页码：541 / 549

页数：9

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