Título:
Synthesis and antiplasmodial assessment of nitazoxanide and analogs as new antimalarial candidates
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Autor:
Irabuena, Camila
Scarone, Laura
Souza, Guilherme Eduardo de
Aguiar, Anna Caroline Campos
Mendes, Giovana Rossi
Guido, Rafael Victorio Carvalho
Serra, Gloria
Scarone, Laura
Souza, Guilherme Eduardo de
Aguiar, Anna Caroline Campos
Mendes, Giovana Rossi
Guido, Rafael Victorio Carvalho
Serra, Gloria
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Artículo
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NITAZOXANIDA
TIAZOL
MALARIA
TIAZOL
MALARIA
Año de publicación:
2022
Contenido:
Resumen:
During the last years, the progression to control malaria disease seems to be slowed and WHO (World Health Organization) reported a modeling analysis with the prediction of the increase in malaria morbidity and mortality in sub-Saharan Africa during the COVID-19 pandemic. A rapid way to the discovery of new drugs could be carried out by performing investigations to identify drugs based on repurposing of “old” drugs. The 5-nitrothiazole drug, Nitazoxanide was shown to be active against intestinal protozoa, human helminths, anaerobic bacteria, viruses, etc. In this work, Nitazoxanide and analogs were prepared using two methodologies and evaluated against P. falciparum 3D7. A bithiazole analog, showed attractive inhibitory activity with an EC50 value of 5.9 μM, low propensity to show toxic effect against HepG2 cells at 25 μM, and no cross-resistance with standard antimalarials.
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Springer
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Medicinal Chemistry Research v. 31, 2022. -- pp. 426–435
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Citación:
Irabuena, C, Scarone, L, Souza, G, y otros. "Synthesis and antiplasmodial assessment of nitazoxanide and analogs as new antimalarial candidates". Medicinal Chemistry Research. [en línea] 2022, vol. 31, pp. 426–435. DOI: https://doi.org/10.1007/s00044-021-02843-1
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Licencia Creative Commons Atribución (CC - By 4.0)
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| Ficheros | Descripción | Tamaño | Formato | ||
|---|---|---|---|---|---|
| AA Irabuena, Camila. Medicinal Chemistry Research v.31, n° 3, 2022. -- pp. 426–435.pdf | — | 1.34 MB | Adobe PDF |