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Type: Artigo de periódico
Title: Synthesis And Preliminary Evaluation Of N-oxide Derivatives For The Prevention Of Atherothrombotic Events.
Author: Rosseto, Leandro Augusto
Pires, Maria Elisa Lopes
Melchior, Aylime Castanho Bolognesi
Bosquesi, Priscila Longhin
Pavan, Aline Renata
Marcondes, Sisi
Chung, Man Chin
Santos, Jean Leandro Dos
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.
Subject: N-oxide
Antiplatelet Activity
Bleeding Time
Rights: aberto
Identifier DOI: 10.3390/molecules201018185
Date Issue: 2015
Appears in Collections:Unicamp - Artigos e Outros Documentos

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