Abstract: Nonsteroidal anti-inflammatory drugs (NSAIDs) 1–5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 1–5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%–61.1% and 65.9%–87.3%, respectively. Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. The inhibitory rates for arachidonic-acid-induced platelet aggregation were similar for compound 2 (80.8%) and acetylsalicylic acid (ASA, 80%). After their oral administration to mice, compounds 1, 3, and 5 showed shorter mean bleeding times than ASA. Compounds 1 and 5 also protected against thromboembolic events, with survival rates of 40% and 33%, respectively, compared with 30% for ASA. In conclusion, these results indicate that these novel NSAIDs containing an NAH subunit may offer better antiplatelet and antithrombotic activities than ASA.
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Chelucci, R.C.; Dutra, L.A.; Lopes Pires, M.E.; de Melo, T.R.F.; Bosquesi, P.L.; Chung, M.C.; dos Santos, J.L. Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit. Molecules 2014, 19, 2089-2099.
Chelucci RC, Dutra LA, Lopes Pires ME, de Melo TRF, Bosquesi PL, Chung MC, dos Santos JL. Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit. Molecules. 2014; 19(2):2089-2099.
Chelucci, Rafael C.; Dutra, Luiz A.; Lopes Pires, Maria E.; de Melo, Thais R.F.; Bosquesi, Priscila L.; Chung, Man C.; dos Santos, Jean L. 2014. "Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit." Molecules 19, no. 2: 2089-2099.