Synthesis and Preliminary Evaluation of N-Oxide Derivatives for the Prevention of Atherothrombotic Events
AbstractThrombosis 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
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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.
Rosseto LA, Pires MEL, Melchior ACB, Bosquesi PL, Pavan AR, Marcondes S, Chung MC, Santos JL. Synthesis and Preliminary Evaluation of N-Oxide Derivatives for the Prevention of Atherothrombotic Events. Molecules. 2015; 20(10):18185-18200.Chicago/Turabian Style
Rosseto, Leandro A.; Pires, Maria E.L.; Melchior, Aylime C.B.; Bosquesi, Priscila L.; Pavan, Aline R.; Marcondes, Sisi; Chung, Man C.; Santos, Jean L. 2015. "Synthesis and Preliminary Evaluation of N-Oxide Derivatives for the Prevention of Atherothrombotic Events." Molecules 20, no. 10: 18185-18200.