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

Abstract

.alpha.-Amino anilides (32) 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. Increased potency was accompanied by increased toxicity. In dogs with surgically induced myocardial infarction 11 compounds were tested; most showed antiarrhythmic activity. 2-Aminopropiono-2'',6''-xylidide, tocainide, was chosen for clinical investigation.