Next Article in Journal
Comparative Evaluation of the Radical-Scavenging Activities of Fucoxanthin and Its Stereoisomers
Previous Article in Journal
Synergism of Cyclin-Dependent Kinase Inhibitors with Camptothecin Derivatives in Small Cell Lung Cancer Cell Lines
Article Menu

Export Article

Open AccessArticle
Molecules 2014, 19(2), 2089-2099;

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)
Full-Text   |   PDF [277 KB, uploaded 18 June 2014]   |  


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. View Full-Text
Keywords: hydrazone; antiplatelet; antithrombotic; NSAIDs; bleeding time hydrazone; antiplatelet; antithrombotic; NSAIDs; bleeding time

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top