1-(4-酰胺基)苄基四氢异喹啉类化合物的合成与生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-(4-ACYLAMINO)-BENZYL-1,2,3,4-TETRAHYDROISOQUINOLINES

异喹啉类化合物有较强的抗高血压、抗心律失常、抗血栓活性。以往对苄基异喹啉的结构改造主要集中于１位和２位，１位取代基为取代的苄基或萘甲基，结构变化不大，而针对２位进行分子设计，合成了许多化合物。研究结果表明，异喹啉母环与１位次甲基连接的芳环在空间构象上...

For searching more effective antiarrhythmic agents, on the basis of integration of the structural feature of certain potassium channel blockers available, various acylamino groups were introduced to the position 4 of the benzyl ring of this series of compounds. Thus, eight 1 (4 acylamino)benzyl 1,2,3,4 tetrahydroisoquinolines were designed and synthesized, which had not been reported in the literatures. Compounds V 1,V 2 and V 6 at concentration 10 -6 mol·L -1 depressed rat aortia contraction induced by high KCl (80 mmol·L -1 ). The effect was similar to that of tetrandrine. Compound V 6 showed potent antiarrhythmic activity at the dosage of 1 mg·kg -1 .