Ferroni R, Simoni D, Manfredini S, Guarneri M, Orlandini P, Barbieri M, Franzè G P, Mugelli A
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Arzneimittelforschung. 1995 Jun;45(6):665-9.
A series of N1-substituted-4-alkoxybenzamidines was synthesized and tested in vitro for their inhibitory effects on blood coagulation and agonist induced platelet aggregation. The antiarrhythmic activity against chloroform-induced arrhythmias in mice was also evaluated. The biological activity of the title compounds is reported in comparison with that of procainamide; among the new products described, IVi and IVe were found to have the most potent anti-platelet and antiarrhythmic activity, respectively. The structure-activity relationships are discussed.
合成了一系列N1-取代的4-烷氧基苯甲脒，并在体外测试了它们对血液凝固和激动剂诱导的血小板聚集的抑制作用。还评估了其对小鼠氯仿诱导的心律失常的抗心律失常活性。报告了标题化合物与普鲁卡因酰胺相比的生物活性；在所描述的新产品中，发现IVi和IVe分别具有最强的抗血小板和抗心律失常活性。讨论了构效关系。
