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Molecules 2015, 20(10), 18185-18200; doi:10.3390/molecules201018185

Synthesis and Preliminary Evaluation of N-Oxide Derivatives for the Prevention of Atherothrombotic Events

1
Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, UNESP, Rodovia Araraquara Jaú Km 01, 14801-902, Araraquara, SP, Brazil
2
Departmento de Farmacologia, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, UNICAMP, Rua Tessália Vieira de Camargon.126, 13083-887, Campinas, SP, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 17 August 2015 / Revised: 5 September 2015 / Accepted: 15 September 2015 / Published: 7 October 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1073 KB, uploaded 7 October 2015]   |  

Abstract

Thrombosis is the main outcome of many cardiovascular diseases. Current treatments to prevent thrombotic events involve the long-term use of antiplatelet drugs. However, this therapy has several limitations, thereby justifying the development of new drugs. A series of N-oxide derivatives (furoxan and benzofuroxan) were synthesized and characterized as potential antiplatelet/antithrombotic compounds. All compounds (3a,b, 4a,b, 8a,b, 9a,b, 13a,b and 14a,b) inhibited platelet aggregation induced by adenosine-5-diphosphate, collagen, and arachidonic acid. All compounds protected mice from pulmonary thromboembolism induced by a mixture of collagen and epinephrine; however, benzofuroxan derivatives (13a,b and 14a,b) were the most active compounds, reducing thromboembolic events by up to 80%. N-oxide derivative 14a did not induce genotoxicity in vivo. In conclusion, 14a has emerged as a new antiplatelet/antithrombotic prototype useful for the prevention of atherothrombotic events. View Full-Text
Keywords: N-oxide; atherothrombosis; antiplatelet activity; bleeding time; furoxan; benzofuroxan; genotoxicity N-oxide; atherothrombosis; antiplatelet activity; bleeding time; furoxan; benzofuroxan; genotoxicity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Rosseto, L.A.; Pires, M.E.L.; Melchior, A.C.B.; Bosquesi, P.L.; Pavan, A.R.; Marcondes, S.; Chung, M.C.; Santos, J.L. Synthesis and Preliminary Evaluation of N-Oxide Derivatives for the Prevention of Atherothrombotic Events. Molecules 2015, 20, 18185-18200.

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