Synthesis of alkylaminoalkylamides of substituted 2-aminopyrroles as potential local anesthetic and antiarrhythmic agents I: alpha-Amines.
The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 19 2-(2-alkylaminoalkylamido)pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, and four showed activity comparable to or greater than that of lidocaine. Most compounds also exhibited antiarrhythmic activity; five compounds had activity comparable to that of lidocaine, and one was more potent. All compounds exhibiting antiarrhythmic activity also were toxic to the central nervous system.
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology; D000779:Anesthetics, Local / Q000138:chemical synthesis*; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D012882:Skin Tests
D000577:Amides; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D011758:Pyrroles