川芎嗪芳酸衍生物的合成及抗血小板聚集活性

有机化学 ›› 2008, Vol. 28 ›› Issue (9): 1578-1583. 上一篇下一篇

研究论文

川芎嗪芳酸衍生物的合成及抗血小板聚集活性

李家明^*,a ; 赵永海^a ; 马逢时^a; 汪志勇^b;何勇^a ; 张德帅^a ; 任海波^a

(a安徽中医学院药学院安徽省现代中药重点实验室合肥 230031)
(b中国科学技术大学化学系合肥 230026)

收稿日期:2008-01-18 修回日期:2008-03-27 发布日期:2008-09-20
通讯作者: 李家明

Synthesis of Ligustrazine-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation

LI, Jia-Ming^*,a ; ZHAO, Yong-Hai^a; MA, Feng-Shi^a; WANG, Zhi-Yong^b
HE, Yong^a; ZHANG, De-Shuai^a; REN, Hai-Bo^a

(a Anhui Key Laboratory of Traditional Chinese Medicine, Department of Pharmacy,
Anhui College of Traditional Chinese Medicine, Hefei 230031)
(b Department of Chemistry, University of Science and Technology of China, Hefei 230026)

Received:2008-01-18 Revised:2008-03-27 Published:2008-09-20
Contact: LI, Jia-Ming

文章分享

摘要/Abstract

以具有活血化淤作用的中药有效成分川芎嗪、阿魏酸为先导物, 按药物化学拼合原理, 设计合成了6个全新结构的川芎嗪芳酸衍生物, 其结构经IR, 1H NMR, 13C NMR及MS确证. 体外药效筛选结果显示, 部分川芎嗪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, 其中川芎嗪阿魏酸拼合物(1a)的抑制活性是奥扎格雷的5.7倍.

关键词: 川芎嗪, 抗血小板聚集, 阿魏酸, 血栓, 川芎嗪芳酸衍生物

Ligustrazine and ferulic acid, which are useful compounds of Chinese traditional medicine, were used as leading compounds. Six ligustrazine-aromatic acid derivatives were designed and synthesized based on the twin drug principle. Their structures were characterized by IR, 1H NMR, 13C NMR and mass spectra. In the in vivo experiment, some compounds have significant inhibitory effect on adenosine diphosphate (ADP) induced platelet aggregation. Among them, the inhibitory effect of compound 1a was 5.7 times than ozagrel.

Key words: ligustrazine, ligustrazine-aromatic acid derivative, platelet aggregation inhibitory, thrombosis, ferulic acid

引用此文

李家明^*,a ; 赵永海^a ; 马逢时^a; 汪志勇^b;何勇^a ; 张德帅^a ; 任海波^a
. 川芎嗪芳酸衍生物的合成及抗血小板聚集活性[J]. 有机化学, 2008, 28(9): 1578-1583.

LI, Jia-Ming^*,a ; ZHAO, Yong-Hai^a; MA, Feng-Shi^a; WANG, Zhi-Yong^b
HE, Yong^a; ZHANG, De-Shuai^a; REN, Hai-Bo^a
. Synthesis of Ligustrazine-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation[J]. Chin. J. Org. Chem., 2008, 28(9): 1578-1583.

导出引用 EndNote|Reference Manager|ProCite|BibTeX|RefWorks

[1]	王子健, 李顺来, 于明武, 骆媛, 王帅, 王永安, 杜洪光. 6-烷氨基-2-乙硫基嘌呤核苷化合物的合成及抗血小板聚集活性研究[J]. 有机化学, 2015, 35(10): 2205-2211.
[2]	夏亚穆, 毕文慧, 王琦, 郭英兰. 倍半木脂素threo-(±)-3,4-二香草基四氢呋喃阿魏酸酯的全合成[J]. 有机化学, 2010, 30(05): 684-690.
[3]	周洲,赖宜生,张奕华,季晖,李立文,彭司勋. 3-芳基-1,2,3,4-噁三唑-5-亚胺与阿司匹林偶联物的合成和抗血栓活性研究[J]. 有机化学, 2008, 28(05): 819-824.
[4]	周洲,蒋丽媛,张奕华,季晖,孙易,彭司勋. 乙酰水杨酰对羟基桂皮酸与呋咱氮氧化物和硝酸酯偶联物的合成及其抗血栓作用[J]. 有机化学, 2006, 26(10): 1403-1408.
[5]	朱万仁, 刘晓珍, 周长军, 雷光清. 新型血栓溶解剂P-6A类似物的合成研究[J]. 有机化学, 2004, 24(9): 1125-1128.
[6]	张治国, 张奕华, 季晖, 邱苏赣. 塞曲司特衍生物的合成和抗哮喘活性[J]. 有机化学, 2004, 24(6): 631-636.

川芎嗪芳酸衍生物的合成及抗血小板聚集活性

Synthesis of Ligustrazine-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation

PDF

可视化

被引次数

摘要/Abstract

引用此文

分享此文

参考文献

相关文章 6

编辑推荐

相关统计

本文评价