Search for New Antiarrhythmic and Hypotensive Compounds. Synthesis, Antiarrhythmic, Antihypertensive, and α‐Adrenoceptor Blocking Activity of Novel 1‐[(2‐Hydroxy‐3‐amino)]‐propylpyrrolidin‐2‐one Derivatives

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Abstract
A series of the derivatives of 1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl]-pyrrolidin-2-one (MG-1) was synthesized and tested for electrocardiographic, antiarrhythmic, and antihypertensive activity as well as for α1- and α2- adrenoceptors binding affinities. Some of the compounds of this series slightly decreased the heart rate, prolonged P-Q, Q-T intervals and QRS complex. Only compound 7 (1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl]-pyrrolidine) possesses potent antiarrhythmic and a slight hypotensive properties, and affinity for α1- and α2- adrenoceptor. The results suggest that the antiarrhythmic and hypotensive effect of compound 7 and MG-1 is related to their adrenolytic properties, and that those properties depend on the presence of a phenylpiperazine moiety.

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