Design, synthesis and antiarrhythmic activity of new amide derivatives of indole-3-carboxylic acid
- Авторлар: Platonova Y.B.1, Tarasov Z.A.1, Volov A.N.1, Volov N.A.2, Savilov S.V.1,3
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Мекемелер:
- Lomonosov Moscow State University
- Pirogov Russian National Research Medical University
- Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences
- Шығарылым: Том 59, № 12 (2023)
- Беттер: 1608-1619
- Бөлім: Articles
- URL: https://ter-arkhiv.ru/0514-7492/article/view/667154
- DOI: https://doi.org/10.31857/S0514749223120054
- EDN: https://elibrary.ru/OEKCFA
- ID: 667154
Дәйексөз келтіру
Аннотация
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.
Негізгі сөздер
Авторлар туралы
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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