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In vitro activity and mechanism of action against the protozoan parasite Trypanosoma cruzi of 5-nitrofuryl containing thiosemicarbazones

Authordc.contributor.authorAguirre, G. 
Authordc.contributor.authorBoiani, Lucía es_CL
Authordc.contributor.authorCerecetto, Hugo es_CL
Authordc.contributor.authorFernández, M. es_CL
Authordc.contributor.authorGonzález, M. es_CL
Authordc.contributor.authorDenicola, Ana es_CL
Authordc.contributor.authorOtero, L. es_CL
Authordc.contributor.authorGambino, Dinorah es_CL
Authordc.contributor.authorRigol Olsen, Carolina es_CL
Authordc.contributor.authorOlea Azar, Claudio es_CL
Authordc.contributor.authorFaúndez Cáceres, Mario Antonio es_CL
Cita de ítemdc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY 12 (18): 4885-4893en_US
Abstractdc.description.abstractThe in vitro growth inhibition activity of new thiosemicarbazone derivatives against the protozoan parasite Trypanosoma cruzi, the causative agent of American trypanosomiasis, are described. The designed compounds combine in the same molecule the thiosemicarbazone function, recently described as a potent cruzain-inhibitor moiety, and the recognised 5-nitrofuryl group, an oxidative stress promoter. Some of the derivatives were found to be very active against the cultured (epimastigote) form of the parasite, being 1.5-1.7-fold more active than the reference compound, Nifurtimox. Free radicals production was detected when the compounds were incubated in presence of mammalian-liver microsomes. The thiosemicarbazones' capacity to act as pharmacophore in the cruzain inhibition process was theoretically analysed. Frontier molecular orbital HOMO was found as an adequate descriptor in this process. Acute in vivo toxicity of two of the more active derivatives was evaluated. The results showed that these compounds are among the most potent 5-nitrofuryl derivatives tested against this parasite thus support further in vivo studies of some of these thiosemicarbazones.en_US
Keywordsdc.subjectNitrofuryl thiosemicarbazonesen_US
Títulodc.titleIn vitro activity and mechanism of action against the protozoan parasite Trypanosoma cruzi of 5-nitrofuryl containing thiosemicarbazonesen_US
Document typedc.typeArtículo de revistaen_US

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