新型胆碱衍生物的合成及其体外抗疟活性

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］。

Synthesis of Novel Choline Derivatives and Their in vitro Antimalarial Activities

Six novel choline derivatives of quaternary ammonium salts(3a~3f) were synthesized by reaction of N,N-dimethyl ethanolamine or N,N-diethyl ethanolamine with brominated alkanes of differ-ent carbon chain length under reflux condition.The structures were characterized by UV-Vis, 1 H NMR and HR-MS.The antimalarial activities test showed that 3a~3f demonstrated different degrees of in-hibiting effect on the growth of plasmodium falciparum 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 ArtemisininIC50(5.7 ±1.54) nmol· L-1].