Guanidinophenyl derivatives of pyrazole: synthesis and inhibitory effect on serine proteinases, blood coagulation and platelet aggregation.
Guanidinophenyl derivatives of pyrazole have been synthesized. Their inhibitory effects on (i) bovine trypsin, bovine thrombin, porcine pancreatic kallikrein catalyzed hydrolysis of p-nitro anilide of N alpha -benzoyl-arginine and (ii) blood coagulation and platelet aggregation, were investigated. The kinetic behaviour of all compounds conformed to that of a reversible competitive inhibition pattern, and they were also found to act in vitro as inhibitors of platelet aggregation induced by ADP.
D000818:Animals; D000925:Anticoagulants / Q000138:chemical synthesis*; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D010450:Endopeptidases; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D010314:Partial Thromboplastin Time; D010974:Platelet Aggregation / Q000187:drug effects*; D011480:Protease Inhibitors; D011517:Prothrombin Time; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D012697:Serine Endopeptidases
D000925:Anticoagulants; D006146:Guanidines; D011480:Protease Inhibitors; D011720:Pyrazoles; D010450:Endopeptidases; D012697:Serine Endopeptidases