农药学学报Issue(2)：136-142,7.DOI:10.3969/j.issn.1008-7303.2015.02.03
7-（1-酰基哌嗪-4-基）甲基喜树碱衍生物的合成及杀虫活性
Synthesis and insecticidal activity of 7-(1-carbonyl-piperazin-4-yl) methyl-camptothecin derivatives
摘要
Abstract
With (20S)-camptothecin (CPT) as the raw material, 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 NMR and LC-MS. The preliminary bioassay showed that the compound 7-( 1-( 4-methoxybenzoyl ) piperazin-4-yl ) methyl-camptothecin ( 4 g ) and 7-( 1-cyclopentanecarbonyl-piperazin-4-yl ) methyl-camptothecin ( 4 j ) exhibited more insecticidal activity against Tetranychus cinnabarinus and Bursaphelenchu xylophilus than CPT. For T. cinnabarinus, LC50 value (24 h) of 4g was 8. 10 and 9. 05 mg/L. And for B. Xylophilus, LC50 (24 h) value of 4j was 6. 34 and 6. 68 mg/L. The results are useful for the investigation of insecticidal activity and structure-activity relationship of camptothecin derivatives.关键词
喜树碱/喜树碱衍生物/朱砂叶螨/松材线虫Key words
camptothecin/camptothecin derivative/Tetranychus cinnabarinus/Bursaphelenchu xylophilus分类
农业科技引用本文复制引用
李忠榜,陈振,陈安良,张绍勇,刘映前,杨波..7-（1-酰基哌嗪-4-基）甲基喜树碱衍生物的合成及杀虫活性[J].农药学学报,2015,(2):136-142,7.基金项目
浙江省重中之重林学一级开放基金(KF201325) （KF201325）
