乙酰水杨酸阿魏酸偶联呋咱和硝酸盐的合成及其抗血栓活性
[Synthesis and antithrombotic activity of acetylsalicyl ferulic acid-coupling furoxans and nitrates].
作者信息
Zhou Zhou, Jiang Li-yuan, Zhang Yi-hua, Ji Hui, Sun Yi, Peng Si-xun
机构信息
Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China.
出版信息
Yao Xue Xue Bao. 2006 Nov;41(11):1050-6.
AIM
To synthesize and study the antithrombotic activity of NO-donating aspirin derivatives.
METHODS
Furoxans and nitrates were incorporated to aspirin via antioxidant ferulic acid as a linker, and the target compounds were screened for in vitro and in vivo inhibitory activities of platelet aggregation, and for inhibitory effect on A-V hypass thromhosis in rats.
RESULTS
Fourteen novel compounds I(1-14), were synthesized and their structures were confirmed Iy MS, IR, 1H NMR and elemental analysis. Biological screening results demonstrated that some tested compounds exhibited potential antithrombotic activ it.
CONCLUSION
Acetylsalicyl ferulic acid-coupling furoxans and nitrates might he used as a lead for further study.
目的
合成并研究含一氧化氮的阿司匹林衍生物的抗血栓活性。
方法
通过抗氧化剂阿魏酸作为连接体将呋咱和硝酸盐与阿司匹林结合，筛选目标化合物对血小板聚集的体外和体内抑制活性，以及对大鼠动静脉旁路血栓形成的抑制作用。
结果
合成了14种新型化合物I(1 - 14)，其结构经质谱、红外光谱、核磁共振氢谱和元素分析确证。生物筛选结果表明，部分受试化合物具有潜在的抗血栓活性。
结论
乙酰水杨酸阿魏酸偶联的呋咱和硝酸盐可作为进一步研究的先导物。
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