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设计合成了一系列2-(4-取代苄基-1,4-高哌嗪-1-基)-N-(5-溴喹喔啉-6-基)乙酰胺化合物,测定其对家兔离体左心房搏出量的影响,对化合物的正性肌力活性进行了初步评价.结果显示,一些衍生物在测试浓度下显示出比上市药物米力农更好的正性肌力活性,其中活性最好的化合物是3f,在浓度为3×10-5mol L-1时,增强左心房搏出量的强度达(6.18±0.06)%[米力农:(2.46±0.07)%].实验中所合成的化合物通过IR,1H NMR,MS和元素分析测试进行了确证.
A series of 2- (4-substituted benzyl 1,4-homopiperazin-1-yl) -N- (5-bromoquinoxalin-6-yl) acetamide compounds were designed and synthesized, In vitro left atrial stroke volume of the impact of compound positive inotropic activity was initially evaluated.The results show that some derivatives at the test concentrations showed better than the listing drug milrinone positive inotropic activity, Among them, the best active compound was 3f, and the intensity of left atrial beating was (6.18 ± 0.06)% [Milrinone: (2.46 ± 0.07)%] when the concentration was 3 × 10-5mol L-1. The compounds synthesized in the experiment were confirmed by IR, 1H NMR, MS and elemental analysis.