Synthesis of 3-amino-4-hydroxy coumarin and dihydroxy-phenyl coumarins as novel anticoagulants


DANIŞ Ö. , Yuce-Dursun B., Gunduz C., OGAN A. , ŞENER G. , Bulut M., ...More

ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, vol.60, no.10, pp.617-620, 2010 (Journal Indexed in SCI) identifier

  • Publication Type: Article / Article
  • Volume: 60 Issue: 10
  • Publication Date: 2010
  • Title of Journal : ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
  • Page Numbers: pp.617-620
  • Keywords: Anticoagulants, 3-Amino-4-hydroxy coumarin, 7,8-Dihydroxy-3-(4-methyl-phenyl)coumarin, 5,7-Dihydroxy-4-phenyl coumarin, Prothrombin time, Warfarin, ORAL ANTICOAGULANTS, DERIVATIVES, PHARMACOGENETICS

Abstract

Natural and synthetic coumarin derivatives have been shown to possess several beneficial pharmacological effects. The anticoagulation and antithrombotic activities of the 4-hydroxy coumarin derivatives are well known. In this study, besides the 4-hydroxy substituent phenyl and p-methylphenyl derivatives were synthesized and confirmed on the basis of their spectral data. 3-Amino-4-hydroxy coumarin, 5,7-dihydroxy-4-phenyl coumarin and 7,8-dihydroxy-3-(4-methyl-phenyl)coumarin were tested in rats to determine whether they had any effect on vitamin K inhibition by investigating the prothrombin time (PT). PT values of coumarin derivatives were compared with those of warfarin (CAS 81-81-2), which is the most commonly used anticoagulant. 7,8-Dihydroxy-3-(4-methylphenyl) coumarin increased PT when compared to saline treated control group and other coumarins synthesized, 3-amino-4-hydroxy coumarin and 5,7-dihydroxy-4-phenyl coumarin.