二苯甲基亚砜基乙酰胺类化合物的设计合成及其抗疲劳活性评价  

Design,Synthesis and Evaluation of Anti-fatigue Activities of Diphenylmethyl Sulfinyl Acetamides

作　　者：陈雷 彭涛 温晓雪 孙云波 刘曙晨 陈肖华 张首国 王林 CHEN Lei;PENG Tao;WEN Xiao-xue;SUN Yun-bo;LIU Shu-chen;CHEN Xiao-hua;ZHANG Shou-guo;WANG Lin(Institute of Radiation Medicine,Academy of Military Medicine Sciences,Academy of Military Sciences,Beijing 100850,China)

机构地区：[1]军事科学院军事医学研究院辐射医学研究所,北京100850

出　　处：《解放军药学学报》2022年第1期12-15,20,共5页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：国家自然科学基金,No.21102176。

摘　　要：目的设计合成具有抗疲劳活性的二苯甲基亚砜基乙酰胺类化合物。方法以莫达非尼为先导化合物设计目标化合物结构,以二苯甲硫基乙酸为起始原料,经过缩合、氧化反应制得目标化合物;通过小鼠转棒疲劳仪评价目标化合物对小鼠运动性疲劳的改善作用。结果成功合成10个目标化合物C_(1)-C_(10),结构经^(1)H-NMR、^(13)C-NMR和HRMS确证,与空白对照组比较,化合物C_(1)、C_(3)、C_(5)、C_(8)具有显著的抗疲劳活性。结论本文设计的化合物合成原料易得、条件温和、操作简便,部分化合物具有显著抗疲劳活性,为深入开展此类结构分子的设计合成及抗疲劳活性研究提供了参考。Objective To design and synthesize diphenylmethyl sulfinyl acetamides with anti-fatigue activities.Methods The structures of target compounds,which were synthesized from diphenylmethylthio-acetic acid via condensation and oxidation,were designed with modafinil as the lead compound.The extent to which target compounds ameliorated exercise-induced fatigue in mice was evaluated by means of a mouse rotary rod fatigue meter.Results Target compounds C_(1)-C_(10) were synthesized and their structures were confirmed by ^(1)H-NMR,^(13)C-NMR and HRMS.C_(1),C_(3),C_(5) and C_(8) showed significant anti-fatigue activities compared to blank control.Conclusion The synthesis method of target compounds requires easily available materials,mild conditions and simple procedures,and four compounds show significant anti-fatigue activities,which provides reference for further study on the design,synthesis and anti-fatigue activities of molecules with similar structures.

关 键 词：莫达非尼 抗疲劳 合成 

分 类 号：R914.5[医药卫生—药物化学]