四氢异喹啉类化合物的合成和抗血小板聚集活性

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。

SYNTHESIS AND ANTIPLATELET AGGREGATION ACTIVITY OF TETRAHYDROISOQUINOLINE COMPOUNDS

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.