Synthesis and class III type antiarrhythmic activity of 4-aroyl (and aryl)-l-aralkylpiperazines.
The synthesis and in vitro Class III antiarrhythmic activity of several 4-aroyl (and aryl)-1-aralkylpiperazine and piperidine derivatives are described. Among several potent compounds identified in the series, RWJ-28810 (3), with its EC20 of 3 nM, ranks as one of the most potent (in vitro) compounds reported.
Kanojia
R M
RM
The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869-0602, USA. rkanojia@pruis.jnj.com
Salata
J J
JJ
Kauffman
J
J
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001681:Biological Assay; D005289:Ferrets; D066298:In Vitro Techniques; D007537:Isometric Contraction / Q000187:drug effects; D008297:Male; D010210:Papillary Muscles / Q000187:drug effects / Q000502:physiology; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology*; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000889:Anti-Arrhythmia Agents; D010879:Piperazines; D010880:Piperidines