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.
Synthesis of N1-substituted benzamidines. Effects on blood coagulation, platelet aggregation and antiarrhythmic activity / R. Ferroni;D. Simoni;S. Manfredini;M. Guarneri;P. Orlandini;M. Barbieri;G. P. Franzè;A. Mugelli. - In: ARZNEIMITTEL-FORSCHUNG. - ISSN 0004-4172. - STAMPA. - 45:(1995), pp. 665-669.