Antiarrhythmic activity of some N-alkylbispidinebenzamides

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Abstract
A series of aromatic ring substituted bispidinebenzamides, 2--10, was prepared by condensation of N-methyl- or N-n-butylbispidine with the appropriate acid chlorides. These compounds were initially evaluated in mice for acute toxicity and for their ability to protect against chloroform-induced ventricular fibrillation. All compounds had significant activity, which was optimized in 2, 3, and 5. These last compounds had potencies and LD50/ED50 ratios comparable to those of a standard antiarrhythmic, disopyramide. However, their potencies in increasing the effective refactory period in isolated rabbit atria were considerably less than that of disopyramide.

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