Antiarrhythmic Mexiletine: A Review on Synthetic Routes to Racemic and Homochiral Mexiletine and its Enantioseparation

Alessia Catalano, Alessia Carocci

doi:10.2174/0929867323666160517120234

摘要

美西律是一类IB级口服抗心律失常药。虽然最初是针对室性心律失常的治疗，但它已被证明对慢性疼痛性糖尿病神经病变，神经性疼痛，骨骼肌离子通道也有治疗作用，最近发现其对肌萎缩侧索硬化症也有作用。本综述详细报道了外消旋体和手性的美西律在近几十年发展起来的不同合成路线，以及手性分离方法和对映体过量测定的分析研究。最后，本文也提到了一些文献中报道的美西律类似物，大部分还介绍了对应的药理研究。

关键词: Antiarrhythmic agents

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Current Medicinal Chemistry

Title:Antiarrhythmic Mexiletine: A Review on Synthetic Routes to Racemic and Homochiral Mexiletine and its Enantioseparation

Volume: 23 Issue: 29

Author(s): Alessia Catalano, Alessia Carocci

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关键词: Antiarrhythmic agents

摘要: Mexiletine is an oral class IB antiarrhythmic agent. Although it was primarily studied for the treatment of ventricular arrhythmias, it has been demonstrated to be useful also for the treatment of chronic painful diabetic neuropathy, neuropathic pain, skeletal muscle channelopathies, and recently amyotrophic lateral sclerosis. This review presents a detailed report on the different synthetic routes to racemic and homochiral mexiletine developed in the last decades, as well as analytical studies regarding enantioseparation methods and enantiomeric excess determination. Finally, some analogues of mexiletine reported in the literature, most of which along with pharmacological studies, have been mentioned.

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Alessia Catalano, Alessia Carocci , Antiarrhythmic Mexiletine: A Review on Synthetic Routes to Racemic and Homochiral Mexiletine and its Enantioseparation, Current Medicinal Chemistry 2016; 23 (29) . https://dx.doi.org/10.2174/0929867323666160517120234

DOI https://dx.doi.org/10.2174/0929867323666160517120234	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X