Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 4, Pages 970-979Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm101198k
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Funding
- Santander-Universidad [GR58/08-921371-891]
- Spanish MEC [CGL2008-03687-E/BOS]
- MCINN [CTQ2009-14288-C04-01, Consolider CSD2010-00065]
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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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