6-(4-酰基-1-哌嗪乙酰氨基)-3,4-二氢-2(1H)-喹啉酮类化合物的合成及正肌力活性初探

目的 :寻找具有正性肌力活性的化合物。方法 :根据文献报道的二氢喹啉酮类正性肌力药物的结构特点 ,设计、合成了其类似物。以苯胺为起始原料经多步合成 ,对所得化合物用离体豚鼠心脏与主动脉观察了心肌收缩力、扩血管作用及心率。结果 :合成了 1 0个 6 ( 4 酰基 1 哌嗪乙酰氨基 ) 3 ,4 二氢 2 ( 1H) 喹啉酮类化合物 ( 4a～ 4j) ,均为未见文献报道的化合物。结论 :初步药理试验表明 ,化合物 ( 4h)显示了正性肌力及扩血管活性。

Synthesis and positive inotropic activities test of 6-(4-acyl-1-piperazinylacetamino)-3,4-dihydro-2(1H)-quinolinone derivatives

OBJECTIVETo search compo undsthat have positive inotropic activities.METHODSAccording to th ereported structures of dihydroquinolinones that have positive inotropic activi ties,aseries of analogues were designed and synthesized.These analogues were sy nthesizedthrough several steps using aniline as a starting material.The biologi cal tests withisolated guinea pig heat and aorta to measure cardiac contractili ty,angiectatic effectsand heart rate.RESULTSTen new compounds of 3 ,4-dihydro6-(4-acyl-1-piperazinyl acetamino)-2(1H)-quino linones(4a～4j) were synthesized.CONCLUSIONPreliminarypharmacologi cal tests showed that 6-(4-benzoyl-1-piperazinylacetamino)-3,4-dihydro-2(1H)-quinolinone(4h) had positive inotropic activity and angiect aic effect.