Journal of Medicinal Chemistry p. 705 - 716 (1992)
Update date:2022-08-02
Topics: Sulfonamides
Ellingboe, John W.
Spinelli, Walter
Winkley, Michael W.
Nguyen, Thomas T.
Parsons, Roderick W.
et al.
The synthesis and Class III antiarrhythmic activity of a series of 4-<(methylsulfonyl)amino>benzamides and sulfonamides are described.Selected compounds shown a potent Class III activity and are devoid of effects on conduction both in vitro (dog Purkinje fibers) and in vivo (anesthetized dogs).Compounds having a 2-aminobenzimidazole group were found to be the most potent, and one compound having the heterocycle (5, WAY-123,398) was selected for further characterization.Compound 5 was shown to have good oral bioavailability and a favorable hemodynamic profile to produce a 3-fold increase of the ventricular fibrillation threshold and to terminate ventricular fibrillation, restoring sinus rhythm in anesthetized dogs.Voltage-clamp studies in isolated myocytes show that 5 is a potent and specific blocker of the delayed rectifier potassium current (IK) at concentrations that cause significant prolongation of action potential duration.
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