Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 1. Heteroarylamine derivatives.
Twenty-four structural derivatives of the antiarrhythmic drug changrolin were synthesized and tested for antiarrhythmic and parasympatholytic activities. It was found that while the bis(pyrrolidinylmethyl)phenol pattern of changrolin appeared to be optimal in this series, a wide latitude existed for the heteroaryl substituent for maintaining good antiarrhythmic activity. Further, the antiarrhythmic and parasympatholytic activities tended to exhibit parallel changes.
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004285:Dogs; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D010276:Parasympatholytics / Q000138:chemical synthesis* / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology
D000889:Anti-Arrhythmia Agents; D010276:Parasympatholytics; D011799:Quinazolines; C022128:changrolin