N-双嘧啶取代芳胺的合成及其抗氧化损伤研究

Synthesis of Bipyrimidine-substituted Aryl Amine Derivatives and Anti-oxidative Damage Assay

报道了一种N-双嘧啶取代芳胺衍生物2-(3-氯苯基)-N-(2-(3-氯苯基)-6-甲基嘧啶-4-基)-N-(2-甲氧苯基)-6-甲基嘧啶-4-胺的合成、表征及其抗氧化生物活性,该N-双嘧啶取代芳胺衍生物是以3-氯苄腈为原料经4步反应合成而得到,其结构通过1HNMR、13CNMR、HR-MS进行了表征和确认。化合物的抗氧化作用与细胞毒作用分别通过是否进行双氧水处理的SH-SY5Y细胞与CCK-8试剂盒进行检测,通过荧光探针DCFH-DA标记检测细胞内ROS含量。结果表明,该化合物具有抗双氧水氧化损伤的可能,能够显著提高细胞存活率且没有明显的细胞毒性。

This work describes the synthesis,characterization of a bipyrimidine-substituted aryl amine derivative 2-（3-chlorophenyl）-N-（2-（3-chlorophenyl）-6-methylpyrimidin-4-yl）-N-（2-methoxyphenyl）-6-methylpyrimidin-4-amine and its anti-oxidative activity.The bipyrimidine-substituted aryl amine derivative is synthesized via four steps reactions starting from 3-chlorobenzonitrile.The structure of the compound was confirmed by1 HNMR,13CNMR and HR-MS.The anti-oxidative effect and cytotoxicity of the compound are tested with CCK-8 assay kit and SH-SY5 Y cells treated with or without hydrogen peroxide.The intracellular accumulation of ROS assay was done with fluorescent probe DCFH-DA.The results suggest that this bipyrimidine-substituted aryl amine derivative is able to protect cells from oxidative stress-induced death and significantly increase the cell viability without evident toxicity.