NEW ANTI-ARRHYTHMIC AGENTS .1. PRIMARY ALPHA-AMINO ANILIDES

Thirty-two α-amino anilides with various substituents in the aromatic ring and in the α 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 α 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. © 1979, American Chemical Society. All rights reserved.