((吡啶-3-基)甲氧基)芳酸衍生物的合成及抗血小板聚集活性  

Synthesis of((pyridin-3-yl)methoxy) aromatic acid derivatives and their inhibitory effects on platelet aggregation

作　　者：李家明[1] 马逢时[1] 龙子江[1] 钟国琛[1] 周鹏[1] 袁明[1] 

机构地区：[1]安徽中医学院药学院安徽省现代中药重点实验室,安徽合肥230031

出　　处：《化学研究与应用》2011年第4期424-430,共7页Chemical Research and Application

基　　金：国家科技重大专项重大新药创制项目(2009ZX09103-123)资助;安徽省高校自然基金重点项目(KJ2010A206)资助

摘　　要：以具有活血化瘀作用的中药有效成分阿魏酸为先导物,按生物电子等排原理,设计合成了6个((吡啶-3-基)甲氧基)芳酸衍生物,其结构经IR,1 H NMR,13 C NMR及MS确证。体外药效筛选结果显示,部分((吡啶-3-基)甲氧基)芳酸衍生物对二磷酸腺苷(ADP)诱导的血小板聚集具有较好的抑制活性,其中化合物1a的抑制作用明显强于阳性对照药奥扎格雷钠。Ferulic acid,which is useful compound of Chinese traditional medicine,was used as leading compound,six（（pyridin-3-yl）methoxy）aromatic acid derivatives were designed and synthesized based on bioisosterism.Their structures were characterized by IR,1H NMR,13C NMR and mass spectra.In vitro experiment,some compounds have good inhibitory effects on adenosine diphophate（ADP） induced platelet aggregation,among them compound 1a showed more potent platelet aggregation inhibitory activity than Ozagrel.

关 键 词：阿魏酸 ((吡啶-3-基)甲氧基)芳酸衍生物 血栓 抗血小板聚集 

分 类 号：O625.51[理学—有机化学]