Design, synthesis and antiarrhythmic activity of new amide derivatives of indole-3-carboxylic acid

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详细

The hERG (human ether-à-go-go-related gene) potassium channel has elicited intense scientific interest due to its counter-intuitive kinetics and its association with arrhythmia and sudden death. Kv1.5 potassium channel, encoded by KCNA5, is a promising target for the treatment of atrial fibrillation, one of the common arrhythmia. A new indole derivatives were synthesized via reaction of indole-3-carboxylic acid with 4-[2-(diethylamino)ethoxy]aniline under peptide coupling protocol in DMF with good yields and evaluated their antiarrythmic activity. Among them, 2-butyl- N -{4-[2-(diethylamino)ethoxy]phenyl}-1-(2-fluorobenzoyl)-1 H -indole-3-carboxamide 34 showed preferable anti-arrhythmic effects and favoured safety. These results indicate that lead compound can be a promising antiarrythmic drug for further studies.

作者简介

Ya. Platonova

Lomonosov Moscow State University

Email: knoposk@gmail.com

Z. Tarasov

Lomonosov Moscow State University

A. Volov

Lomonosov Moscow State University

N. Volov

Pirogov Russian National Research Medical University

S. Savilov

Lomonosov Moscow State University;Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences

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