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咪唑芳酸衍生物的合成及抗血小板聚集活性
引用本文:周鹏,何勇,李家明,许勤龙,盛日正. 咪唑芳酸衍生物的合成及抗血小板聚集活性[J]. 中国现代应用药学, 2011, 28(5): 446-450
作者姓名:周鹏  何勇  李家明  许勤龙  盛日正
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,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);安徽省自然科学基金项目(070413118)
摘    要:
目的合成4个咪唑芳酸衍生物。方法以香草酸、丁香酸为起始原料,经Williamson醚化、亲核取代和水解反应,合成咪唑芳酸衍生物4 a~4 d。结果目标化合物的结构经IR、1H-NMR、13C-NMR及MS确证。结论初步的药理实验结果显示,在12 mmol·L-1浓度下,化合物4 a的血小板抑制率达到84.5%。

关 键 词:咪唑芳酸衍生物  抗血小板聚集  合成
收稿时间:2010-08-12

Synthesis of Imidazole-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation
ZHOU Peng,HE Yong,LI Jiaming,XU Qinlong and SHENG Rizheng. Synthesis of Imidazole-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation[J]. The Chinese Journal of Modern Applied Pharmacy, 2011, 28(5): 446-450
Authors:ZHOU Peng  HE Yong  LI Jiaming  XU Qinlong  SHENG Rizheng
Affiliation:ZHOU Peng,HE Yong,LI Jiaming*,XU Qinlong,SHENG Rizheng(Department of Pharmacy,Anhui College of Traditional Chinese Medicine,Anhui Key Laboratory of Traditional Chinese Medicine,Hefei 230031,China)
Abstract:
OBJECTIVE To synthesize four new compounds of imidazole-aromatic acid derivatives. METHODS Imidazole-aromatic acid derivatives were prepared from vanillic acid, syringic acid via Williamson etherification, nucleophilic substitution, and hydroxylation. RESULTS The structures of the target compounds were confirmed by IR, 1H-NMR, 13C-NMR and MS. CONCLUSION Preliminary pharmacological results showed that the inhibitory effect on platelet aggregation of compound 4a at 12 mmol·L-1 was 84.5%.
Keywords:imidazole-aromatic acid derivatives   platelet aggregation inhibitory   synthesis
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