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

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.