摘要
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。
OBJECTIVE:To search compounds that have positive inotropic activities.METHODS:According to the reported structures of dihydroquinolinones that have positive inotropic activities,a series of analogues were designed and synthesized.These analogues were synthesized through several steps using aniline as a starting material.The biological tests with isolated guinea pig heat and aorta to measure cardiac contractility,angiectatic effects and heart rate.RESULTS:Ten new compounds of 3,4 dihydro 6 (4 acyl 1 piperazinyl acetamino) 2(1H) quinolinones(4a～4j) were synthesized.CONCLUSION:Preliminary pharmacological tests showed that 6 (4 benzoyl 1 piperazinylacetamino) 3,4 dihydro 2(1H) quinolinone(4h) had positive inotropic activity and angiectaic effect.
出处
《中国现代应用药学》
CSCD
2000年第3期206-208,共3页
Chinese Journal of Modern Applied Pharmacy
基金
吉林省科委资助课题!第 95 35 46号
关键词
正性肌力作用
强心药
二氢喹啉酮
合成
positive inotropic activity
cardiotonics
dihydroquinolinone
synthesis
