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Molecules 2014, 19(2), 2089-2099; doi:10.3390/molecules19022089

Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit

Departamento de Fármacos e Medicamentos, Faculdade de Ciências Farmacêuticas–UNESP, Rodovia Araraquara Jaú Km, Araraquara, SP, 01, 14801-902, Brazil
* Author to whom correspondence should be addressed.
Received: 8 November 2013 / Revised: 30 January 2014 / Accepted: 10 February 2014 / Published: 17 February 2014
(This article belongs to the Section Medicinal Chemistry)
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Nonsteroidal anti-inflammatory drugs (NSAIDs) 15 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 15 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.
Keywords: hydrazone; antiplatelet; antithrombotic; NSAIDs; bleeding time hydrazone; antiplatelet; antithrombotic; NSAIDs; bleeding time
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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