鬼臼毒素类似物结构与杀虫活性关系初探Ⅱ.构效关系分析及理想结构推测

以鬼臼毒素为原料合成了一系列衍生物。用质谱和核磁共振鉴定这些化合物的结构和构型 ,测定了其对 5龄菜青虫 (Pierisrapae)、3龄小菜蛾 (Plutella xylostella)和 3龄粘虫 (Mythimna separata)的生物活性。结果表明 ,具反式内酯环的鬼臼衍生物活性显著高于具顺式内酯环的衍生物 ,4位取代基对杀虫活性影响较大 ;推测出了较为理想的鬼臼毒素类似物杀虫活性物质的结构通式。

Study on the relationship between structure and insecticidal activity of podophyllotoxin analogues

Some derivatives of podophyllotoxin were synthesised and characterized.Their bioactivity against Pieris rapae,Plutella xylostella and Mythimna separata were detected.The result showed that the relationship between structure of podophyllotoxin analogues and their insecticidal activity was very obvious.The derivatives with trans-lactone ring were more active than those of cislactone ring.The substituent of C-4 might influence its bioactivity greatly.A common structure which was considered to be of highly insecticidal activity was inferred.