Synthesis, anticoagulant and PIVKA-II induced by new 4-hydroxycoumarin derivatives.
The action of the coumarin-type drugs and related compounds is reviewed to their VKOR antagonistic effects. In our study, twenty 3-pyridinyl, pyrimidinyl and pyrazolyl-4-hydroxycoumarin derivatives were synthesized. A comparative in vivo (CT, PT determination) and in vitro (measurement of PIVKA-II levels) anticoagulant study with respect to warfarin showed that the synthesized compounds have different anticoagulant activities, the most prospective compounds were the 3-pyrazolyl-4-hydroxycoumarin derivatives.
Abdelhafez
Omaima M
OM
Department of Chemistry of Natural Products, National Research Center, Dokki, Cairo, Egypt. ommryan@yahoo.com
Amin
Kamelia M
KM
Batran
Rasha Z
RZ
Maher
Timothy J
TJ
Nada
Somaia A
SA
Sethumadhavan
Shalini
S
D015110:4-Hydroxycoumarins / Q000737:chemistry* / Q000494:pharmacology; D000284:Administration, Oral; D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000600:supply & distribution; D015415:Biomarkers; D003374:Coumarins / Q000008:administration & dosage / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D007928:Lethal Dose 50; D015394:Molecular Structure; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011498:Protein Precursors / Q000494:pharmacology*; D011516:Prothrombin / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014859:Warfarin / Q000494:pharmacology*
D015110:4-Hydroxycoumarins; D000925:Anticoagulants; D015415:Biomarkers; D003374:Coumarins; D010975:Platelet Aggregation Inhibitors; D011498:Protein Precursors; C008208:acarboxyprothrombin; D014859:Warfarin; D011516:Prothrombin; C030123:coumarin; C068805:4-hydroxycoumarin