Produção Nacional
Revisado por pares
Diacetal Ditellurides as Highly Active and Selective Antiparasitic Agents toward Leishmania amazonensis
2019; American Chemical Society; Volume: 10; Issue: 5 Linguagem: Inglês
10.1021/acsmedchemlett.9b00060
ISSN1948-5875
AutoresPamela T. Bandeira, João Pedro A. Souza, Débora B. Scariot, Francielle Pelegrin Garcia, Celso Vataru Nakamura, Alfredo R. M. Oliveira, Leandro Piovan,
Tópico(s)Macrophage Migration Inhibitory Factor
ResumoLeishmaniasis is a neglected tropical disease and a public health concern in at least 98 countries, affecting mainly the poorest populations. Pharmaceuticals and chemotherapies available for leishmaniasis treatment have several limitations, which clearly justify the efforts to find new potential antileishmanial drugs. In this context, antiprotozoal activities toward different Leishmania species have been reported for hypervalent tellurium compounds, which motivated us to investigate, for the first time, the leishmanicidal properties of some nonhypervalent diaryl ditellurides. Thus, this work describes in vitro activity against Leishmania amazonensis and the cytotoxicities of diaryl ditellurides. Ditelluride LQ7 revealed a strong leishmanicidal activity on promastigotes and amastigotes at submicromolar levels (IC50 = 0.9 ± 0.1 and 0.5 ± 0.1 μmol L-1, respectively) and presented selectivity indexes greater than those of reference drug miltefosine. This preliminary study suggests that diaryl ditellurides may be promising scaffolds for the development of new agents for leishmaniasis treatment.
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