郁敏, 华维一, 彭司勋. 四氢异喹啉类化合物的合成和抗血小板聚集活性J. 药学学报, 1995, 30(2): 112-118.
引用本文: 郁敏, 华维一, 彭司勋. 四氢异喹啉类化合物的合成和抗血小板聚集活性J. 药学学报, 1995, 30(2): 112-118.
M Yu, WY Hua , SX Peng, . SYNTHESIS AND ANTIPLATELET AGGREGATION ACTIVITY OF TETRAHYDROISOQUINOLINE COMPOUNDSJ. Acta Pharmaceutica Sinica, 1995, 30(2): 112-118.
Citation: M Yu, WY Hua , SX Peng, . SYNTHESIS AND ANTIPLATELET AGGREGATION ACTIVITY OF TETRAHYDROISOQUINOLINE COMPOUNDSJ. Acta Pharmaceutica Sinica, 1995, 30(2): 112-118.

四氢异喹啉类化合物的合成和抗血小板聚集活性

SYNTHESIS AND ANTIPLATELET AGGREGATION ACTIVITY OF TETRAHYDROISOQUINOLINE COMPOUNDS

  • 摘要: 某些异喹啉化合物有抗血小板聚集活性,如喘速宁的纯光学异构体R-(+)体有较明显的抗血小板聚集作用。本文重点对四氢异喹啉母核(I1~I4)的2位进行取代基修饰,共合成了14个化合物。体外药理筛选结果初步表明,大部分化合物有一定的抗血小板聚集活性,其中II3,II5,II7,II8和II10活性较强。

     

    Abstract: In an attempt to search for novel antiplatelet aggregation agents,14 newcompounds(II1~II14 ) were synthesized on the basis of the structure feature of β-adrenergic agonistTrimetoquinol and found whose R-(+)-isomer is more potent than other agents used clinically. Allthese compounds were not reported in literature previously.Their chemical structures were determinedby elemental analysis, MS, 1HNMR and IR. Preliminary pharmacological results showed that most of the compounds were active on ADP-induced platelet aggregation in mice(in vitro), among which II3,II5,II7,II8 and II10 have strongerinhibitory activity.

     

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