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  • Title: In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
    Author: Sánchez-Moreno M, Sanz AM, Gómez-Contreras F, Navarro P, Marín C, Ramírez-Macias I, Rosales MJ, Olmo F, Garcia-Aranda I, Campayo L, Cano C, Arrebola F, Yunta MJ.
    Journal: J Med Chem; 2011 Feb 24; 54(4):970-9. PubMed ID: 21229977.
    Abstract:
    The in vivo trypanosomicidal activity of the imidazole-based benzo[g]phthalazine derivatives 1-4 and of the new related pyrazole-based compounds 5 and 6 has been studied in both the acute and chronic phases of Chagas disease. As a rule, compounds 1-6 were more active and less toxic than benznidazole in the two stages of the disease, and the monosubstituted derivatives 2, 4, and 6 were more effective than their disubstituted analogs. Feasible mechanisms of action of compounds 1-6 against the parasite have been explored by considering their inhibitory effect on the Fe-SOD enzyme, the nature of the excreted metabolites and the ultrastructural alterations produced. A complementary histopathological analysis has confirmed that the monosubstituted derivatives are less toxic than the reference drug, with the behavior of the imidazole-based compound 4 being especially noteworthy.
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