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 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.
D000813:Anilides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis*; D001281:Atrial Fibrillation / Q000517:prevention & control; D002725:Chloroform / Q000633:toxicity; D003331:Coronary Vessels / Q000187:drug effects; D004285:Dogs; D005260:Female; D051379:Mice
D000813:Anilides; D000889:Anti-Arrhythmia Agents; D002725:Chloroform