【摘要】 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。更多还原

【Abstract】 With( 20S)-camptothecin( CPT) as the rawmaterial,a series of 7-( 1-carbonyl-piperazin-4-yl) methyl-camptothecin derivatives( 4a-4m) were synthesized after modification of C7 of CPT.Their structures were identified by1 H NM R and LC-M S. The preliminary bioassay showed that the compound 7-( 1-( 4-methoxybenzoyl) piperazin-4-yl) methyl-camptothecin( 4g) and 7-( 1-cyclopentanecarbonyl-piperazin-4-yl) methyl-camptothecin( 4j) exhibited more insecticidal activity against Tetranychus cinnabarinus and Bursaphelenchu xylophilus than CPT. For T. cinnabarinus,LC50value( 24 h) of 4g was 8. 10 and 9. 05 mg / L. And for B. Xylophilus,LC50( 24 h) value of 4j was6. 34 and 6. 68 mg / L. The results are useful for the investigation of insecticidal activity and structureactivity relationship of camptothecin derivatives.更多还原