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. |
| ZHOU Peng,HE Yong,LI Jiaming,XU Qinlong,SHENG Rizheng.Synthesis of Imidazole-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(5):446-450. |
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摘要: |
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 |
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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) |
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Synthesis of Imidazole-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation |
ZHOU Peng,HE Yong,LI Jiaming,XU Qinlong,SHENG Rizheng
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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%. |
Key words: imidazole-aromatic acid derivatives platelet aggregation inhibitory synthesis |