1-(4-烃氧基)苄基四氢异喹啉类化合物及相关化合物的合成与生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-(4-ALKYLOXY)BENZYL-1,2,3,4-TETRAHYDROISOQUINOLINES AND RELATED COMPOUNDS

摘要: 以有心血管活性的异喹啉生物碱为先导物,设计合成了15个3,4-二氢(II_1,2)和1,2,3,4-四氢-(4-烃氧基)苄基四氢异喹啉化合物(II_3～15)。药理实验表明:大部分化合物有舒张血管条作用,其中化合物II₉对低钾诱导的血管收缩有较强的抑制作用,而对高钾诱导的血管收缩无作用,对硝酸乌头碱诱发的大鼠室性心律失常有明显保护作用。

Abstract: In an attempt to search for novel cardiovascular drugs which might act on calcium or potassium channels, on the basis of the previous study of our group,15 1-(4-alkyloxy)benzyl-1,2,3,4-tetrahydroisoquinolines derivatives were designed and synthesized among which 10 were not reported previously in the literature.Preliminary pharmacological studies showed that most of these compounds exhibited relaxation of rat thoria aorta in vitro. Compound III₉ exhibited potent inhibiting action on low KCl(20 mmol·L^-1)-induced contraction of rat aorta, and significant protective effect on experimental arrhythmia in rats.