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为研究喜树碱(CPT)类化合物的杀线虫活性,以喜树碱为原料,经烷基化、氧化、酯化等步骤合成了13个7-C-取代的20-(S)-喜树碱衍生物,其中化合物14未见文献报道,所有衍生物的结构经红外光谱(FT-IR)、核磁共振氢谱(1H NMR)和液-质联用(LC-MS)等分析手段进行了表征。采用浸渍法测定了化合物对松材线虫Bursaphelenchus xylophilus的毒杀活性。结果表明:与母体化合物喜树碱相比,7-C-取代的20-(S)-喜树碱衍生物具有更强的杀线虫活性,其中化合物7-苄基喜树碱、7-甲酰基喜树碱、7-苯甲酰氧甲基喜树碱在24 h的致死中浓度(LC50值)分别为2.28、2.21和1.37 mg/L,明显高于母体化合物喜树碱的LC50值12.18 mg/L。
In order to study the nematicidal activity of camptothecin (CPT) compounds, 13 7-C-substituted 20- (S) -cyclodextrins were synthesized by the steps of alkylation, oxidation and esterification with camptothecin The structures of all the derivatives were analyzed by FT-IR, 1H NMR and LC-MS methods. However, Characterization. The toxicity of the compound to Bursaphelenchus xylophilus was determined by impregnation method. The results show that 7-C-substituted 20- (S) -camptothecin derivatives have stronger nematicidal activity than the parent compound camptothecin, in which the compounds 7-benzylcamptothecin, 7- The LC50 values of acyl camptothecin and 7-benzoyloxymethyl camptothecin at 24 h were 2.28, 2.21 and 1.37 mg / L, respectively, which were significantly higher than the LC50 value of camptothecin of parent compound 12.18 mg / L.