Review Article

电压门控钠通道阻滞剂:美西律类似物和同系物的合成

卷 28, 期 8, 2021

发表于: 04 May, 2020

页: [1535 - 1548] 页: 14

弟呕挨: 10.2174/0929867327666200504080530

价格: $65

摘要

美西律汀是一种属于IB类的抗心律不齐药物,起钠通道阻滞剂的作用。除了其对心律不齐的众所周知的活性外,其在治疗肌强直,肌强直性营养不良和肌萎缩性侧索硬化症方面的效用现已广为人知。但是,由于其不良作用,它已从多个国家退出市场。因此,在过去的几年中,有几篇论文报道了美西律的类似物和同系物具有更宽的治疗率和更强的选择性。其中一些显示出钠通道阻断活性高于母体化合物。值得注意的是,尽管广泛证明了两种对映体的活性存在差异,美西律汀仍以消旋体的形式用于治疗,但(-)-(R)-对映体的活性更高:这一发现促使多个研究小组进行了美西律汀的研究。及其旋光形式的类似物和同系物。这篇综述总结了用于获得这些化合物的不同合成途径。它们可能代表了新的类似美西律的化合物的有趣起点,而没有与使用美西律有关的常见副作用。

关键词: 抗心律不齐药,抗肌强直药,钠通道阻滞剂,美西律类似物,美西律同源物,肌萎缩性侧索硬化症(ALS)。

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