Synthesis of alkylaminoalkylamides of substituted 2-aminopyrroles as potential local anesthetic and antiarrhythmic agents. II: beta-Amines.
The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 14 2-(3-alkylaminoalkylamido)-pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, with seven showing comparable or greater activity than lidocaine. Most compounds also exhibited antiarrhythmic activity; three compounds had more potent activity than lidocaine. All compounds exhibiting antiarrhythmic activity also were toxic to the CNS. However, two of the three compounds having greater activity than lidocaine possessed more desirable therapeutic indexes.
D000588:Amines / Q000138:chemical synthesis* / Q000494:pharmacology; D000779:Anesthetics, Local / Q000138:chemical synthesis* / Q000633:toxicity; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000633:toxicity; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D007928:Lethal Dose 50; D051379:Mice; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology
D000588:Amines; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D011758:Pyrroles