摘要
以吲哚美辛（１）为原料先经酯化反应和Ｋｎｏｅｖｅｎａｇｅｌ缩合，再与可溶性淀粉连接，合成了侧链含有阿魏酸的高分子载体药物（４），该化合物未见文献报道．用比浊法和放免法测定了（４）体外对兔血小板聚集以及对ＴＸＢ２，６ＫｅｔｏＰＧＦ１α含量的影响．化合物（４）２４０μｍｏｌ·Ｌ－１对ＡＡ诱导的兔血小板聚集的抑制率为３９６％，对ＴＸＢ２释放的抑制率为２８７％．与吲哚美辛（１）或阿魏酸比较，阿魏酸衍生物高分子载体药物（４）显示有抑制兔体外血小板聚集和抑制ＴＸＢ２，６ＫｅｔｏＰＧＦ１α释放的作用，呈现明显的药物协同作用．
The polymeric drug(FAIS) which contains ferulic acid(FA) was synthesized from indomethacin via esterfication and the Knoevenagel condensation,and then conjunction with soluble starch(S).This new compound was obtained for the first time.The results of preliminary pharmacological tests showed that the FAIS could inhibit the rabbit platelet aggregation induced by arachidonic acid(AA) and release of TXB2 and 6KetoPGF1.Its activity was stronger than that of FA and indomethacin.It was in evidence to express the good synergic effect.
出处
《中国药物化学杂志》
CAS
CSCD
1999年第2期98-101,共4页
Chinese Journal of Medicinal Chemistry
关键词
阿魏酸
吲哚美辛
高分子载体
血小板聚集
ferulic acid
indomethacin
polymeric drug
platelet aggregation
