摘要
目的：寻找新型的心血管药物。方法：根据推理药物设计原理，设计合成目标化合物，并研究其生物活性。结果：合成了１６个川芎哚的类似物（Ｉ～ＸＶＩ），其中８个化合物（Ｉ，Ｉ，Ｖ～ＶＩ，ＩＸ，ＸＩ和ＸＶ）是新化合物。结论：所合成的川芎哚类似物均有一定程度的抗血小板聚集作用，其中Ｉ～ＩＶ，ＶＩ，Ｘ，ＸＩ及ＸＩＩ有一定程度的抗血栓作用。
AIM: To search for compounds for the treatment of cardiovascular diseases. METHODS: According to rational drug design principle, a series of analogues of perlolyrine were prepared, and the antiplatelet aggregation activity and antithrombotic effects of these compounds were tested. RESULTS: Sixteen perlolyrine analogues were synthsized(I～XVI). Of them, 8 compounds(I,II,V～VII,IX,XI and XV) were first reported. CONCLUSION: All synthesized compounds showed antiplatelet aggregation activity to a certain degree. Of them, 8 compounds(I～IV,VII,X,XI and XIII) exhibited antithrombotic effects.
出处
《药学学报》
CAS
CSCD
北大核心
1999年第7期498-504,共7页
Acta Pharmaceutica Sinica
基金
高等学校博士学科点专项科研基金
国家自然科学基金
关键词
川芎哚
结构改造
抗血小板聚集
抗血栓
perlolyrine
structural modification
antiplatelet aggregation
antithrombotic effects
