吴茱萸碱衍生物的合成与抗弓形虫活性研究  

Study on the synthesis and anti-toxoplasma activity of evodiamine derivatives

作　　者：李智红[1] 周勇[1] 孙玉桥 全哲山 方应权[1] LI Zhi-hong;ZHOU Yong;SUN Yu-qiao;QUAN Zhe-shan;FANG Ying-quan(Chongqing Three Gorges Medical College,Chonqing 404120,China;Affiliated Hospital,Yanbian University,Yanji 133002,China)

机构地区：[1]重庆三峡医药高等专科学校,重庆404120 [2]延边大学附属医院,吉林延吉133002

出　　处：《化学研究与应用》2021年第9期1730-1736,共7页Chemical Research and Application

基　　金：重庆市教委科技项目(KJQN201902711)资助;重庆三峡医药高等专科学校项目(2018xzyb03)资助。

摘　　要：本文以吴茱萸碱为先导化合物,设计合成了8种新型吴茱萸碱衍生物。所有衍生物经过^(1)H NMR、^(13)C NMR、MS和IR进行结构确认,并采用MTT测定法测定所有化合物对宿主细胞(HeLa)的细胞毒性以及对弓形虫感染的HeLa细胞的半数抑制浓度,并计算选择性指数(SI)。所有化合物均表现出较强的抗弓形体作用,其中化合物B1显示出最低的细胞毒性和最强的抗弓形体作用。化合物B1的SI值为1.53,优于阳性对照螺旋霉素、磺胺嘧啶和乙胺嘧啶,以及先导化合物吴茱萸碱。In this paper,eight novel evodiamine derivatives were designed and synthesized using evodiamine as the lead compound.The structure of all derivatives was confirmed by ^(1)H NMR,^(13)C NMR,MS and IR.The cytotoxicity of all compounds to host cells(HeLa)and the half inhibitory concentration of HeLa cells infected with Toxoplasma gondii were determined by the MTT assay,and the selectivity index(SI)was calculated.All compounds showed strong anti-Toxoplasma gondii effect,among which compound B1 showed the lowest cytotoxicity and strongest anti-Toxoplasma gondii effect.SI value of compound B1 was 1.53,which was better than the positive control spiramycin,sulfadiazine and pyrimethamine,and the lead compound evodiamine.

关 键 词：吴茱萸碱 合成 抗弓形虫 喹啉 三唑 

分 类 号：O626[理学—有机化学]