Progress toward the development of a safe and effective agent for treating reentrant cardiac arrhythmias: synthesis and evaluation of ibutilide analogues with …

…, MW McMillan, SC Perricone, DM Squires…

Index: Hester; Gibson; Buchanan; Cimini; Clark; Emmert; Glavanovich; Imbordino; LeMay; McMillan; Perricone; Squires; Walters Journal of Medicinal Chemistry, 2001 , vol. 44, # 7 p. 1099 - 1115

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Citation Number: 25

Abstract

A series of ibutilide analogues with fluorine substituents on the heptyl side chain was prepared and evaluated for class III antiarrhythmic activity, metabolic stability, and proarrhythmic potential. It was found that fluorine substituents stabilized the side chain to metabolic oxidation. Many of the compounds also retained the ability to increase the refractoriness of cardiac tissue at both slow and fast pacing rates. The potential for ...