New antiarrhythmic agents. 1. Primary .alpha.-amino anilides

Thirty-two alpha-amino anilides with various substituents in the aromatic ring and in the alpha position are described. Their abilities to protect mice against chloroform-induced fibrillation and to elicit toxicity were determined. Substitution of an alkyl or aryl group in the alpha position enhance...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1979-10, Vol.22 (10), p.1171-1176
Main Authors: Byrnes, Eugene W, McMaster, Paul D, Smith, Emil R, Blair, Murray R, Boyes, R. Nichol, Duce, Benjamin R, Feldman, Hal S, Kronberg, George H, Takman, Bertil H, Tenthorey, Paul A
Format: Article
Language:English
Subjects:
Anilides - chemical synthesis
Anilides - pharmacology
Animals
Anti-Arrhythmia Agents - chemical synthesis
Atrial Fibrillation - prevention & control
Chloroform - toxicity
Coronary Vessels - drug effects
Dogs
Female
Mice
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Summary:Thirty-two alpha-amino anilides with various substituents in the aromatic ring and in the alpha position are described. Their abilities to protect mice against chloroform-induced fibrillation and to elicit toxicity were determined. Substitution of an alkyl or aryl group in the alpha position enhanced the antifibrillatory activity. In most cases, increased potency was accompanied by increased toxicity. Eleven compounds were tested in dogs with surgically induced myocardial infarction; most showed antiarrhythmic activity. 2-Aminopropiono-2',6'-xylidide, tocainide, was chosen for clinical investigation.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00196a005