Ruenitz P C, Mokler C M
J Med Chem. 1979 Sep;22(9):1142-4. doi: 10.1021/jm00195a030.
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.
通过N-甲基或N-正丁基联吡啶与适当的酰氯缩合，制备了一系列芳环取代的联吡啶苯甲酰胺，即2 - 10。最初在小鼠中对这些化合物进行了急性毒性以及预防氯仿诱导的心室颤动能力的评估。所有化合物都具有显著活性，其中2、3和5的活性最佳。这最后几种化合物的效能和LD50/ED50比值与标准抗心律失常药丙吡胺相当。然而，它们在增加离体兔心房有效不应期方面的效能远低于丙吡胺。
