Paper
Synthesis and antiarrhythmic activity of alpha-[(diarylmethoxy)methyl]-1-piperidineethanols.
Published 1991 · M. Hoefle, L. T. Blouin, Robert W. Fleming
Journal of medicinal chemistry
5
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Abstract
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.
Alpha-[(diarylmethoxy)methyl]-1-piperidineethanols show promising antiarrhythmic activity, with 2,6-dimethylpiperidine being essential for long-lasting action and quaternary ammonium salts not being essential for long-term action.
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