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., ...Daha Fazla

ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, cilt.60, sa.10, ss.617-620, 2010 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 60 Sayı: 10
  • Basım Tarihi: 2010
  • Dergi Adı: ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED)
  • Sayfa Sayıları: ss.617-620
  • Anahtar Kelimeler: 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
  • Marmara Üniversitesi Adresli: Evet

Özet

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.