| 摘要: |
| 【目的】寻找具有更高杀虫活性的新型多杀菌素衍生物。【方法】 以盐酸水解获得的多杀菌素C-9假糖苷配基为受体，以3种单糖（D-葡萄糖、D-半乳糖、L-鼠李糖）为供体，采用三氯乙酰亚胺法进行糖苷化反应得到C-9位不同糖基大环内酯类衍生物；用核磁共振谱（1H-NMR、13C-NMR），MS和IR对所合成衍生物进行表征，并分别测定所合成衍生物的杀虫活性。【结果】1H-NMR、13C-NMR、MS和IR谱图分析表明，新合成的3种多杀菌素衍生物分别为9-0-(β-D-吡喃葡萄糖)多杀菌素衍生物、9-0-(β-D-吡喃半乳糖)多杀菌素衍生物、9-0-(β-L-吡喃鼠李糖)多杀菌素衍生物；杀虫活性测定表明，3种新型多杀菌素衍生物在20 mg/L剂量下对锯谷盗、赤拟谷盗、米蛾等均表现出一定的杀虫活性，致死率为31%～59%。【结论】新合成的多杀菌素衍生物均具有一定的杀虫活性，其构效关系还具有进一步研究的价值。 |
| 关键词: 多杀菌素 糖基衍生物 杀虫活性 |
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| 基金项目:国家粮食公益性行业科研专项“储粮虫霉监测与生态控制技术研究”（201313002） |
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| Synthesis and insecticidal activity of different aglycones derivatives of spinosad C-9 |
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WANG Xu,CHEN Xin,LI Long,et al
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| Abstract: |
| 【Objective】The purpose of this study was to synthesize spinosad with better insecticidal activity.【Method】Using C-9 aglycone as receptor and three monosaccharaides (D-gluclse,D-galactose,and L-rhamnose) as donor,different aglycones derivatives of spinosad C-9 were synthesized using trichloroacetimidate method.All compounds were confirmed by 1H-NMR,13C-NMR,MS and IR and their insecticidal activities were determined.【Result】Spectra analysis with 1H-NMR,13C-NMR,MS and IR confirmed that the new synthesized three derivatives were 9-0 (β-D-pyran glucose),9-0-(β-D-pyran galactose),and 9-0-(β-L-pyran rat lee sugar).The new compounds exhibited intertidal activities against Oryzaephilus surinamensis,Tribolium castaneum (Herbst),Corcyra cephalonica at concentration of 20 mg/L,and the lethality was 31%-59%.【Conclusion】The compounds synthesized in this study had good insecticidal activity and the structure activity relationship should be further studied. |
| Key words: spinosad glycosyl derivatives insecticidal activity |
