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Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/123456789/305

Título : Synthesis and Antimalarial Activity of Ethyl 3-Amino-4-oxo-9- (phenylsubstituted)thieno[2,3-b]quinoline-2-carboxylate Derivatives.
Autor : Charris, Jaime
Barazarte, Arthur
Domínguez, José
Lobo, Gricela
Camacho, José
Ferrer, Rosa
Gamboa, Neira
Rodrigues, Juan
Fecha de publicación : May-2007
Editorial : Heterocyclic Chem.,
Resumen : A series of thieno[2,3-b]quinolone derivatives were synthesized and investigated for their abilities to inhibit 􀀁-hematin formation, hemoglobin hydrolysis and in vivo for their efficacy in rodent Plasmodium berghei. Compound 3b was the most promising as inhibitor of hemoglobin hydrolysis, and its effects as inhibitor of 􀀁-hematin formation was promising. When the aromatic ring was substituted in 2 (Me), in 3 (CF3) or in 2,4 (Cl) the inhibition of hemoglobin proteolysis was maximal (88%), the rest of compounds maintained a low inhibition. The most active compound to emerge in vitro and in murine studies, was 3b suggesting an antimalarial activity via multiple mechanisms.
URI : http://saber.ucv.ve/123456789/305
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