7-取代-4,5-二氢-[1,2,4]噁二唑并[4,3-a]喹啉-1-酮的合成及负性肌力作用评价。
Synthesis and negative inotropic effects evaluation of 7-substituted-4,5-dihydro-[1,2,4]oxadiazolo[4,3-a]quinolin-1-ones.
机构信息
Department of Physiology, College of Basic Medical Sciences, Yanbian University, Yanji, 133000, Jilin, People's Republic of China.
出版信息
Arch Pharm Res. 2013 Nov;36(11):1338-44. doi: 10.1007/s12272-013-0203-6. Epub 2013 Aug 6.
A series of 7-alkoxy-4,5-dihydro-[1,2,4]oxadiazolo[4,3-a]quinolin-1-ones was synthesized and their negative inotropic effects were evaluated by measuring the left atrium stroke volume in isolated rabbit heart preparations. All compounds moderated the cardiac workload by decreasing heart rate and contractility (inotropic effects). Among them, compound 6 was found to be best potent with a -28.89 ± 1.91 % decrease in the stroke volume at a concentration of 3 × 10(-5) M in our in vitro study.
合成了一系列 7-烷氧基-4,5-二氢-[1,2,4]噁二唑并[4,3-a]喹啉-1-酮，并通过测量离体兔心标本中的左心房冲程体积来评估其负性肌力作用。所有化合物均通过降低心率和收缩力（肌力作用）来调节心脏工作量。其中，在我们的体外研究中，化合物 6 在 3 × 10(-5) M 的浓度下使冲程体积减少了-28.89 ± 1.91%，显示出最佳的效力。
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