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Novel arylpyrazino[2,3-c][1,2,6]thiadiazine 2,2-dioxides as inhibitors of platelet aggregation. 1. Synthesis and pharmacological evaluation

AutorCampillo, Nuria E. ; García, Concepción; Goya, Pilar ; Páez, Juan A. ; Carrasco, Emilio; Grau, Manuel
Fecha de publicación20-may-1999
EditorAmerican Chemical Society
CitaciónJournal of Medicinal Chemistry 42 (10) : 1698–1704 (1999)
ResumenA series of N-1-substituted derivatives of pyrazino[2,3-c][1,2,6]thiadiazine 2,2-dioxides bearing aryl groups at the pyrazino moiety have been prepared. The synthesis involves ring formation between the diaminothiadiazine and suitable dicarbonyl compounds and subsequent introduction of the substituent at N-1. The compounds have been tested in vitro, as inhibitors of rabbit and human platelet aggregation, and ex vivo against rat platelet aggregation induced by arachidonic acid, ADP, collagen, U46619, and I-BOP. The results obtained indicate that some pyrazino[2,3-c][1,2,6]thiadiazine derivatives show significant platelet aggregation inhibition similar to other antithrombotic agents and that the antiplatelet properties may be mediated by interference with the arachidonic acid pathway
Versión del editorhttp://dx.doi.org/10.1021/jm981103j
URIhttp://hdl.handle.net/10261/44653
DOI10.1021/jm981103j
ISSN0022-2623
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