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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
Chelucci, Rafael Consolin [1] ; Dutra, Luiz Antonio [1] ; Lopes Pires, Maria Elisa [1] ; Ferreira de Melo, Thais Regina [1] ; Bosquesi, Priscila Longhin [1] ; Chung, Man Chin [1] ; dos Santos, Jean Leandro [1]
Total Authors: 7
Affiliation:
[1] UNESP, Fac Ciencias Farmaceut, Dept Farmacos & Med, BR-14801902 Araraquara, SP - Brazil
Total Affiliations: 1
Document type: Journal article
Source: Molecules; v. 19, n. 2, p. 2089-2099, FEB 2014.
Web of Science Citations: 16
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. (AU)

FAPESP's process: 12/50359-2 - Design, synthesis and pharmacological evaluation of new hybrid drugs useful to treat hematological disorders
Grantee:Jean Leandro dos Santos
Support Opportunities: Research Grants - Research Partnership for Technological Innovation - PITE
FAPESP's process: 11/15204-5 - Synthesis and Pharmacological Evaluation of new hybrid compounds useful to treat sickle cell disease symptoms
Grantee:Thaís Regina Ferreira de Melo
Support Opportunities: Scholarships in Brazil - Master