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((吡啶-3-基)甲氧基)芳酸衍生物的合成及抗血小板聚集活性
引用本文:李家明,马逢时,龙子江,钟国琛,周鹏,袁明. ((吡啶-3-基)甲氧基)芳酸衍生物的合成及抗血小板聚集活性[J]. 化学研究与应用, 2011, 23(4): 424-430
作者姓名:李家明  马逢时  龙子江  钟国琛  周鹏  袁明
作者单位: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
基金项目: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,1H NMR,13C 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...

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

Synthesis of((pyridin-3-yl)methoxy) aromatic acid derivatives and their inhibitory effects on platelet aggregation
LI Jia-ming,MA Feng-shi,LONG Zi-jiang,ZHONG Guo-chen,ZHOU Peng,YUAN Ming. Synthesis of((pyridin-3-yl)methoxy) aromatic acid derivatives and their inhibitory effects on platelet aggregation[J]. Chemical Research and Application, 2011, 23(4): 424-430
Authors:LI Jia-ming  MA Feng-shi  LONG Zi-jiang  ZHONG Guo-chen  ZHOU Peng  YUAN Ming
Affiliation:LI Jia-ming,MA Feng-shi,LONG Zi-jiang,ZHONG Guo-chen,ZHOU Peng,YUAN Ming(Anhui Key Laboratory of Traditional Chinese Medicine,Department of Pharmacy,Anhui University of Traditional Chinese Medicine,Hefei 230031,China)
Abstract: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.
Keywords:ferulic acid  ((pyridin-3-yl)methoxy)aromatic acid derivatives  thrombosis  platelet aggregation inhibition  
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