| Abstract: | Anticoagulant 4-Hydroxy-2-pyrones Twenty-seven derivatives of 4-hydroxy-2H-pyran-2-one were synthesized and tested for their anticoagulant and blood platelet aggregation inhibiting activity. After oral administration of a single dose of 330 mg/kg to rats, prothrombin levels below 25 % were seen with 14 compounds. These values were reached after almost 12 h and maintained up to 48 h. Maximum activity is observed between 24 and 36 h. The most active compound 11 shows therapeutic prothrombin levels even after administration of 100 mg/kg. The 4-hydroxy-2-pyranone 1 and the corresponding 4-hydroxycumarine 28 show similar activity. Four compounds were weak platelet aggregation inhibitors (5 · 10?4 M). |
