嘧啶核苷-查尔酮杂化体的合成及其抗利什曼原虫活性研究

Synthesis and Antileishmanial Activity of Pyrimidine NucleosideChalcone Hybrids

以5-甲酰基嘧啶核苷为原料,经与(取代)苯乙酮缩合,得到了一系列含有嘧啶核苷和查尔酮两种优势结构单元的杂化体.生物活性研究结果表明,其中的一些杂化体具有显著的抗利什曼原虫活性,从而为新药的开发提供了有价值的先导化合物和构效关系信息.

In this paper, a group of pyrimidine nucleoside-chalcone hybrids were conveniently prepared through condensing 5-formyl pyrimidine nucleosides with（substituted） acetophenones under the promotion of aqueous sodium hydroxide. The hybrid compounds were then evaluated as potential antileishmanial agents and some of them showed promisingly potent activities.