Synthesis,bioactivities and 3D-QSAR of novel avermectin B2a aglycon derivatives  

作　　者：Fangfang Huang Huan Ling Jiao Li Sen Lu Weijie Liu Qingshan Li Fengbo Xu 

机构地区：[1]State Key Laboratory of Elemento-Organic Chemistry,Department of Chemistry,College of Chemistry,Nankai University

出　　处：《Chinese Chemical Letters》2020年第1期141-144,共4页中国化学快报（英文版）

基　　金：supported by the National Key R&D Program of China (No.2018YFD0200100)

摘　　要：Fourteen avermectin B2 a aglycon derivatives were designed and synthesized after removing the oleandrose disaccharide of avermectin B2 a.Their structures were characterized by’H NMR,13 C NMR,HMRS.Preliminary bioassays indicated that these compounds exhibited good insecticidal activity against diamondback moth at 200 mg/L,with mortality no less than 90%.Compounds 10 b,12 a,12 c,17 demonstrated good acaricidal activity against the adult mites,larvae,and good inhibition rate of hatching to mite eggs of Tetranychus cinnabarinus.Compounds 5,10 b,10 c exhibited excellent fungicidal activity against fourteen fungal pathogens in vitro.3 D-QSAR analysis showed that the fungicidal activity of avermectin B2 a aglycon derivatives would be increased when a negatively charged and bulky group was introduced at 13-position,which will be instructive for the further modification of avermectin B2 aaglycon.Fourteen avermectin B2 a aglycon derivatives were designed and synthesized after removing the oleandrose disaccharide of avermectin B2 a.Their structures were characterized by ’H NMR,13 C NMR,HMRS.Preliminary bioassays indicated that these compounds exhibited good insecticidal activity against diamondback moth at 200 mg/L,with mortality no less than 90%.Compounds 10 b,12 a,12 c,17 demonstrated good acaricidal activity against the adult mites,larvae,and good inhibition rate of hatching to mite eggs of Tetranychus cinnabarinus.Compounds 5,10 b,10 c exhibited excellent fungicidal activity against fourteen fungal pathogens in vitro.3 D-QSAR analysis showed that the fungicidal activity of avermectin B2 a aglycon derivatives would be increased when a negatively charged and bulky group was introduced at 13-position,which will be instructive for the further modification of avermectin B2 aaglycon.

关 键 词：Avermectin B2a aglycon Biological activity INSECTICIDE ACARICIDE FUNGICIDE 3D-QSAR 

分 类 号：TQ450.1[化学工程—农药化工]