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以(20S)-喜树碱(CPT)为原料,根据类同合成法和亚结构连接法原理,对CPT的7-C位进行修饰,得到了系列新型7-(1-酰基哌嗪-4-基)甲基喜树碱衍生物(4a~4m),所有衍生物的结构均通过核磁共振氢谱(1H NM R)和液-质联用(LC-M S)等方法确证;并初步测定了其对朱砂叶螨Tetranychus cinnabarinus和松材线虫Bursaphelenchu xylophilus的室内杀虫活性。结果表明:与喜树碱相比,各衍生物均表现出不同程度的杀虫活性,其中化合物7-[1-(4-甲氧基苯酰基)哌嗪-4-基]-甲基喜树碱(4g)和7-(1-环戊酰基哌嗪-4-基)-甲基喜树碱(4j)对朱砂叶螨24 h的半数致死浓度(LC50值)分别为8.10和9.05 mg/L,对松材线虫的LC50值分别为6.34和6.68 mg/L。研究结果可为喜树碱衍生物杀虫活性构效关系研究奠定基础。
A series of novel 7- (1-acylpiperazin-4-yl) -piperidin-4-one derivatives of CPT were modified with (20S) -camptothecin - yl) methyl camptothecin derivatives (4a ~ 4m). The structures of all the derivatives were confirmed by 1H NMR and LC-MS methods. The indoor insecticidal activities against tetranychus cinnabarinus and Bursaphelenchu xylophilus were determined. The results showed that each derivative showed different degree of insecticidal activity compared with camptothecin. The compound 7- [1- (4-methoxyphenoyl) piperazin-4-yl] -methyl The median lethal concentration (LC50) of trichlorfon (4g) and 7- (1-cyclopentanopiperazin-4-yl) -methyl camptothecin (4j) for Tetranychus cinnabarinus for 24 h were 8.10 and 9.05 mg / L, and the LC50 values for pine wood nematode were 6.34 and 6.68 mg / L, respectively. The results provide a basis for the study of the structure-activity relationship of camptothecin derivatives.