title: Guanidinophenyl derivatives of pyrazole: synthesis and inhibitory effect on serine proteinases, blood coagulation and platelet aggregation.
abstract: 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.
mesh_terms: 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
chemical_list: D000925:Anticoagulants; D006146:Guanidines; D011480:Protease Inhibitors; D011720:Pyrazoles; D010450:Endopeptidases; D012697:Serine Endopeptidases