Synthesis and antiarrhythmic activity of .alpha.-[(diarylmethoxy)methyl]-1-piperidineethanols

A series of alpha-[(diarylmethoxy)methyl]-1-piperidineethanols was evaluated for antiarrhythmic activity in the coronary artery ligated dog model. Structure-activity relationship studies indicated that the 2,6-dimethylpiperidine group afforded the best antiarrhythmic agents in this series and was es...

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Veröffentlicht in:	Journal of medicinal chemistry 1991-01, Vol.34 (1), p.7-12
Hauptverfasser:	Hoefle, Milton L, Blouin, L. T, Fleming, R. W, Hastings, S, Hinkley, J. M, Mertz, T. E, Steffe, T. J, Stratton, C. S, Werbel, L. M
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Arrhythmia Agents - chemical synthesis Benzyl Compounds - chemical synthesis Benzyl Compounds - chemistry Benzyl Compounds - pharmacology Chemistry Coronary Vessels - physiology Dogs Exact sciences and technology Heart Rate - drug effects Heterocyclic compounds Heterocyclic compounds with only one n hetero atom and condensed derivatives Molecular Structure Organic chemistry Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Preparations and properties Structure-Activity Relationship
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Zusammenfassung:	A series of alpha-[(diarylmethoxy)methyl]-1-piperidineethanols was evaluated for antiarrhythmic activity in the coronary artery ligated dog model. Structure-activity relationship studies indicated that the 2,6-dimethylpiperidine group afforded the best antiarrhythmic agents in this series and was essential for long duration of action. This investigation indicated that quaternary ammonium salts were not essential for a long duration of action. It was also shown that the antiarrhythmic activity could be separated from the tachycardia frequently caused by this type of agent.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00105a002