Synthesis and Antiarrhythmic Activity of N-[2-(Adamantan-2-YL)Aminocarbonyl-Methyl-N′-(Dialkylamino)Alkylnitrobenzamides

Novel 2-aminoadamantane derivatives, specifically N-[2-(adamant-2-yl)-aminocarbonylmethyl]-N′-(dialkylamino) alkylnitrobenzamides and their physiologically compatible salts, preferably the hydrochlorides, were synthesized and their pharmacological properties were studied. The novel derivatives were...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2019-04, Vol.53 (1), p.23-28
Main Authors: Avdyunina, N. I., Turilova, A. I., Gan’shina, T. S., Mirzoyan, R. S., Grushevskaya, L. N., Zaitseva, N. M., Pyatin, B. M.
Format: Article
Language:English
Subjects:
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
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Summary:Novel 2-aminoadamantane derivatives, specifically N-[2-(adamant-2-yl)-aminocarbonylmethyl]-N′-(dialkylamino) alkylnitrobenzamides and their physiologically compatible salts, preferably the hydrochlorides, were synthesized and their pharmacological properties were studied. The novel derivatives were found to have marked antiarrhythmic (antifibrillatory) activity in models of calcium chloride and aconitin arrhythmia. The relationship between the chemical structures of the substances synthesized here and their pharmacological activities was studied. The highest level of antiarrhythmic activity and the lowest toxicity were obtained with compound N-[2-(adamant-2-yl)aminocarbonylmethyl]-N′-[3-diethylamino]propyl]-4-nitrobenzamide, which also had the advantage of a wider therapeutic ratio over known antiarrhythmic drugs of classes I, IV, and III (cardiocyclide).
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-019-01949-6