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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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咪唑芳酸衍生物的合成及抗血小板聚集活性
周鹏1, 何勇1, 李家明1, 许勤龙1, 盛日正1
安徽中医学院药学院,安徽省现代中药重点实验室,合肥 230031
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
DOI:
分类号:
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)
Synthesis of Imidazole-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation
ZHOU Peng,HE Yong,LI Jiaming,XU Qinlong,SHENG Rizheng
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
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