Banitt E H, Coyne W E, Schmid J R, Mendel A
J Med Chem. 1975 Nov;18(11):1130-4. doi: 10.1021/jm00245a017.
Benzamides and naphthamides characterized by one or more 2,2,2-trifluoroethoxy ring substituents have been prepared and evaluated as antiarrhythmic agents in mice. Structure-action studies reveal that antiarrhythmic activity is highly dependent upon the number and position of 2,2,2-trifluoroethoxy groups. The most potent compounds are derived from 2,5-bis(2,2,2-trifluoroethoxy)benzamide, and, within this group, wide variation of the amide side chain is possible without adversely affecting the antiarrhythmic activity.
已制备出以一个或多个2,2,2-三氟乙氧基环取代基为特征的苯甲酰胺和萘甲酰胺，并在小鼠中作为抗心律失常药物进行了评估。构效关系研究表明，抗心律失常活性高度依赖于2,2,2-三氟乙氧基的数量和位置。最有效的化合物衍生自2,5-双(2,2,2-三氟乙氧基)苯甲酰胺，并且在该组内，酰胺侧链可以有很大变化而不会对抗心律失常活性产生不利影响。
