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Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani
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 IC(50) values ranging from 2 to 45 µm. The most active tetraoxane, compound LC140, exhibited an I...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7038143/ https://www.ncbi.nlm.nih.gov/pubmed/31979089 http://dx.doi.org/10.3390/molecules25030465 |
Sumario: | 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 IC(50) values ranging from 2 to 45 µm. The most active tetraoxane, compound LC140, exhibited an IC(50) 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. |
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