3,8-Diazabicyclo-[3.2.1]-octane derivatives as analogues of ambasilide, a Class III antiarrhythmic agent

Stefania Villa, Daniela Barlocco, Giorgio Cignarella, Gyula Julius Papp, Beáta Baláti, János Takács, András Varró, András Borosy, Katalin Keserû, Péter Mátyus

Research output: Contribution to journalArticlepeer-review


Ambasilide, a representative of Class III antiarrhythmics, was reported to prolong the cardiac action potential duration in the dog, with little or no effect on Ca and Na currents. We synthesised a series of ambasilide analogues, having the 3,8-diazabicyclo-[3.2.1]-octane moiety instead of the 3,7-diazabicyclo-[3.3.1]-nonane present in ambasilide. The compounds were tested both in vitro extracellular electrophysiological assays and by the conventional microelectrode technique. Most of them lengthened the effective refractory period (ERP) with no change or slight increase on the impulse conduction time (ICT). Similarly some of the tested compounds lengthened the action potential duration (APD), a typical Class III feature, without exerting any significant effect on the maximal rate of depolarization, therefore apparently lacking Class I antiarrythmic activity.

Original languageEnglish
Pages (from-to)495-506
Number of pages12
JournalEuropean Journal of Medicinal Chemistry
Issue number6
Publication statusPublished - Jun 1 2001


  • Ambasilide
  • Antiarrhythmic activity
  • Diazabicyclo-[3.2.1]-octane

ASJC Scopus subject areas

  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science


Dive into the research topics of '3,8-Diazabicyclo-[3.2.1]-octane derivatives as analogues of ambasilide, a Class III antiarrhythmic agent'. Together they form a unique fingerprint.

Cite this