新型喜树碱类药性分子的合成与杀螨活性

Synthesis and acaricidal activity of novel camptothecin-inspired heterocycle scaffolds

应用三组分"一锅法"合成了一系列新型喜树碱类药性分子4a^4n、5a^5n和7a^7f,所有目标化合物均经核磁共振氢谱和质谱确证。室内杀螨活性测定结果表明,所有化合物对朱砂叶螨Tetranychus cinnabarinus均有不同程度的杀螨活性,其中化合物4l(LC_(50):25.93 mg/L)和7d(LC_(50):28.16 mg/L)的杀螨活性与喜树碱(LC_(50):24.55 mg/L)的相当。该研究为进一步开展喜树碱作为先导的新农药设计与研究提供了基础。

A new series of camptothecin-inspired heterocycle scaffolds were prepared utilizing a three component one-pot synthetic protocol. Their structures were characterized by ~1H NMR and LC-MS. The acaricidal activities against Tetranychus cinnabarinus were further tested. All the synthesized compounds exhibited different degree of acaricidal activities. Especially, the LC_（50） values of compounds 4l and 7d against T. cinnabarinus were 25.93 mg/L and 28.16 mg/L, respectively, which were very similar to that of camptothecin（24.55 mg/L）. Our study provides a basis for the further development of novel insecticide with camptothecin as the lead compound.