Guanidinophenyl derivatives of pyrazole: synthesis and inhibitory effect on serine proteinases, blood coagulation and platelet aggregation

Farmaco Sci. 1986 Oct;41(10):747-57.

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

  • Animals
  • Anticoagulants / chemical synthesis*
  • Cattle
  • Chemical Phenomena
  • Chemistry
  • Endopeptidases
  • Guanidines / chemical synthesis*
  • Guanidines / pharmacology
  • Humans
  • Partial Thromboplastin Time
  • Platelet Aggregation / drug effects*
  • Protease Inhibitors*
  • Prothrombin Time
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Serine Endopeptidases

Substances

  • Anticoagulants
  • Guanidines
  • Protease Inhibitors
  • Pyrazoles
  • Endopeptidases
  • Serine Endopeptidases