Synthesis of N1-substituted benzamidines. Effects on blood coagulation, platelet aggregation and antiarrhythmic activity.
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.
Ferroni
R
R
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Simoni
D
D
Manfredini
S
S
Guarneri
M
M
Orlandini
P
P
Barbieri
M
M
Franzè
G P
GP
Mugelli
A
A
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology; D001550:Benzamidines / Q000138:chemical synthesis* / Q000494:pharmacology; D004594:Electrophysiology; D006321:Heart / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D010314:Partial Thromboplastin Time; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D012756:Sheep; D013329:Structure-Activity Relationship
D000889:Anti-Arrhythmia Agents; D000925:Anticoagulants; D001550:Benzamidines; D010975:Platelet Aggregation Inhibitors