Abstract

The hERG potassium channel has recently received increased scientific interest due to its association with arrhythmia and sudden death from cardiovascular disease. The Kv1.5 channel, encoded by the KCNA5 gene, is a promising biotarget for the treatment of atrial fibrillation, one of the common arrhythmias. This work describes the synthesis of new amide derivatives of indole-3-carboxylic acid through its reaction with 4-[2-(diethylamino)ethoxy]aniline under the conditions of peptide synthesis in N,N-dimethylformamide. The target compounds were obtained in good yields, and their structure was studied by ¹H NMR spectroscopy, mass spectrometry, and thermogravimetric analysis. The synthesized compounds were tested for antiarrhythmic activity.

中文翻译：

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新型吲哚-3-甲酰胺衍生物的设计、合成及抗心律失常活性

摘要

hERG 钾通道最近因其与心律失常和心血管疾病猝死的相关性而受到越来越多的科学关注。由 KCNA5 基因编码的 Kv1.5 通道是治疗房颤（常见心律失常之一）的有前途的生物靶标。该工作描述了在N , N-二甲基甲酰胺中肽合成的条件下，通过与4-[2-(二乙基氨基)乙氧基]苯胺的反应，合成了吲哚-3-羧酸的新型酰胺衍生物。以良好的收率获得了目标化合物，并通过¹ H NMR 谱、质谱和热重分析研究了其结构。测试合成的化合物的抗心律失常活性。