New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides
作者:Paul A. Tenthorey、H. Jack Adams、George H. Kronberg、Bertil H. Takman
DOI:10.1021/jm00141a008
日期:1981.9
A series of 2,3-diaminopropionanilides was synthesized by acylation of mono- and disubstituted aniline derivatives with 2,3-dibromopropionyl chloride and subsequent amination with the appropriate secondary amines. The target compounds were evaluated in mice for antiarrhythmic efficacy against chloroform-induced tachycardia and for central nervous system toxicity. Several of the active agents were found
通过用2,3-二溴丙酰氯将单和二取代的苯胺衍生物酰化并随后用适当的仲胺胺化,合成了一系列的2,3-二氨基丙酰苯胺。在小鼠中评估了目标化合物对氯仿诱导的心动过速的抗心律失常功效以及中枢神经系统毒性。发现几种活性剂比利多卡因具有更高的抗心律失常功效,但它们也有毒。以大鼠坐骨神经阻滞的形式评估目标化合物的局部麻醉活性表明,大多数化合物的阻滞时间与利多卡因相似。没有一个依替卡因具有长期的阻断作用。