Antiplatelet and antithrombotic activities of non-steroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit.

摘要: Nonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet antithrombotic activities assessed in vitro vivo. Compounds inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% 65.9%-87.3%, respectively. 1 5 most active compounds, inhibiting adenosine-diphosphate-induced 57.2% 61.1%, The inhibitory for arachidonic-acid-induced similar compound 2 (80.8%) acetylsalicylic acid (ASA, 80%). After oral administration to mice, compounds 1, 3, showed shorter mean bleeding times than ASA. also protected against thromboembolic events, survival 40% 33%, respectively, compared 30% In conclusion, these results indicate that novel NSAIDs NAH may offer better