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Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/123456789/304

Título : Synthesis and antimalarial activity of pyrazolo and pyrimido benzothiazine dioxide derivatives
Autor : Barazarte, Arthur
Lobo, Gricela
Gamboa, Neira
Rodrigues, Juan R.
Capparelli, Mario V.
Álvarez-Larena, Ángel
López, Simón E.
Charris, Jaime E.
Palabras clave : Benzothiazines
Pyrazol
Pyrimidine
Plasmodium berghei
b-Hematin
Hemoglobin
Fecha de publicación : 27-Jun-2011
Resumen : A series of phenylsubstituted pyrazolo and pyrimido benzothiazine dioxide derivatives were synthesized and investigated for their abilities to inhibit b-hematin formation, hemoglobin hydrolysis and in vivo for their antimalarial efficacy in rodent Plasmodium berghei. Compounds 3-amino-7-chloro-9-(20-methylpheyl)- 1,9-dihydro-pyrazolo-[4,3-b]benzothiazine 4,4-dioxide 2b and 2,4-diamino-8-chloro-10Hphenyl- pyrimido-[5,4-b]benzothiazine 5,5-dioxide 3a were the most promising as inhibitors of hemoglobin hydrolysis, however, their effect as inhibitors of b-hematin formation was marginal, except for compound 3-amino-7-chloro-9-(30-chlorophenyl)-1,9dihydro-pyrazolo-[4,3-b]benzothiazine 4,4-dioxide 2g. The most active compound to emerge from the in vitro and in vivo murine studies was 2b, suggesting an antimalarial activity via inhibition of hemoglobin hydrolysis, however, not as efficient as chloroquine.
URI : http://saber.ucv.ve/123456789/304
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