新型胆碱衍生物的合成及其体外抗疟活性

Synthesis of Novel Choline Derivatives and Their in vitro Antimalarial Activities

以N,N-二甲基乙醇胺和N,N-二乙基乙醇胺为初始原料,分别与不同碳链长度的溴代烷烃回流反应合成了6个新型的季铵盐型胆碱衍生物(3a^3f),其结构经UV-Vis,1H NMR和HR-MS表征。初步抗疟活性测试结果表明:3a^3f对恶性疟原虫3D7的增殖均有一定的体外抑制活性,(1-羟基)二乙基正丁基溴化铵(3f)的活性最强[IC50(68.1±6.5)nmol·L-1],但低于青蒿素[IC50(5.7±1.54)nmol·L-1]。

Six novel choline derivatives of quaternary ammonium sahs（3a - 3f） were synthesized by reaction of N,N-dimethyl ethanolamine or N,N-diethyl ethanolamine with brominated alkanes of different carbon chain length under reflux condition. The structures were characterized by UV-Vis, ^1H NMR and HR-MS. The antimalarial activities test showed that 3a - 3f demonstrated different degrees of inhibiting effect on the growth of plasmodiumfalciparum 3D7 in vitro, and （1-hydroxy） diethyl n-butyl ammonium bromide （3f） exhibited the strongest antimalarial activity with IC50 of （68.1 ± 6.5 ） nmol · L^-1, but lower than Artemisinin[ IC50（5.7 ± 1.54） nmol · L^-1 ].