Article Dans Une Revue Molecules Année : 2020

Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani

Résumé

A chemically diverse range of novel tetraoxanes was synthesized and evaluated in vitro against intramacrophage amastigote forms of Leishmania donovani. All 15 tested tetraoxanes displayed activity, with IC50 values ranging from 2 to 45 µm. The most active tetraoxane, compound LC140, exhibited an IC50 value of 2.52 ± 0.65 µm on L. donovani intramacrophage amastigotes, with a selectivity index of 13.5. This compound reduced the liver parasite burden of L. donovani-infected mice by 37% after an intraperitoneal treatment at 10 mg/kg/day for five consecutive days, whereas miltefosine, an antileishmanial drug in use, reduced it by 66%. These results provide a relevant basis for the development of further tetraoxanes as effective, safe, and cheap drugs against leishmaniasis.

Dates et versions

hal-05149167 , version 1 (07-07-2025)

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Lília Cabral, Sébastien Pomel, Sandrine Cojean, Patrícia Amado, Philippe Loiseau, et al.. Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani. Molecules, 2020, 25 (3), pp.465. ⟨10.3390/molecules25030465⟩. ⟨hal-05149167⟩
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