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Rutaecarpine衍生物的合成及体外抗血小板聚集活性
引用本文:刘青,郑伟,桑海婴,陈建兴. Rutaecarpine衍生物的合成及体外抗血小板聚集活性[J]. 中国药物化学杂志, 2006, 16(1): 20-22
作者姓名:刘青  郑伟  桑海婴  陈建兴
作者单位:1. 国家新药筛选中心,上海,201203
2. 上海市计划生育科学研究所,药物研究室,上海,200032
摘    要:目的合成新的rutaecarpine衍生物并对其抗血小板聚集活性进行研究。方法先合成rutaecarpine,再进行N-取代反应,合成目标化合物,并测试所合成化合物的体外抗血小板聚集活性。结果与结论共合成6个未见文献报道的新化合物,它们的结构经1H-NMR和MS确证。初步体外药理实验结果显示:有4个新化合物对血小板聚集的抑制作用强于母体化合物rutaecarpine。

关 键 词:药物化学  化合物制备  化学合成  rutaecarpine衍生物  抗血小板聚集
文章编号:1005-0108(2006)01-0020-03
收稿时间:2005-09-19
修稿时间:2005-09-19

Synthesis and anti-platelet aggregation activities in vitro of rutaecarpine derivatives
LIU Qing,ZHENG Wei,SANG Hai-ying,CHEN Jian-xing. Synthesis and anti-platelet aggregation activities in vitro of rutaecarpine derivatives[J]. Chinese Journal of Medicinal Chemistry, 2006, 16(1): 20-22
Authors:LIU Qing  ZHENG Wei  SANG Hai-ying  CHEN Jian-xing
Affiliation:1. The National Center for Drug Screening, Shanghai 201203, China ; 2. Department Drug Research, Shanghai Institute of Planned Parenthood Research, Shanghai 200032, China
Abstract:Aim To design and synthesize new rutaecarpine derivatives,and to evaluate their activities of anti-platelet aggregation.Methods Rutaecarpine was prepared,then the target compounds were synthesized from rutaecarpine via N-substitution.Their anti-platelet aggregation activities were determined in vitro.Results and conclusions Six derivatives of rutaecarpine were synthesized with the structures confirmed by their()~1H-NMR and MS spectra.The primary pharmacological test in vitro shows that the anti-platelet aggregation activities of four new derivatives are higher than that of rutaecarpine.
Keywords:medicinal chemistry  compound preparation  chemical synthesis  rutaecarpine derivatives  anti-platelet aggregation
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