Título:
Multi-anti-parasitic activity of arylidene ketones and thiazolidene hydrazines against trypanosoma cruzi and Leishmania spp.
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Autor:
Álvarez, Guzmán
Perdomo, Cintya
Coronel, Cathia
Aguilera, Elena
Varela, Javier
Aparicio Díaz, Hector Gonzalo
Zolessi, Flavio R.
Cabrera, Nallely
Vega, Celeste
Rolón, Miriam
Rojas de Arias, Antonieta
Pérez-Montfort, Ruy
Cerecetto, Hugo
González, Mercedes
Perdomo, Cintya
Coronel, Cathia
Aguilera, Elena
Varela, Javier
Aparicio Díaz, Hector Gonzalo
Zolessi, Flavio R.
Cabrera, Nallely
Vega, Celeste
Rolón, Miriam
Rojas de Arias, Antonieta
Pérez-Montfort, Ruy
Cerecetto, Hugo
González, Mercedes
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Tipo de documento:
Artículo
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Palabras clave:
Anti-T. cruzi and anti-Leishmania spp. activity
Arylidene ketones
Thiazolidene hydrazines
Triosephosphate isomerase
Cruzipain
In vivo toxicity
Zebrafish
Arylidene ketones
Thiazolidene hydrazines
Triosephosphate isomerase
Cruzipain
In vivo toxicity
Zebrafish
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Año de publicación:
2017
Contenido:
Resumen:
A series of fifty arylideneketones and thiazolidenehydrazines was evaluated against Leishmania infantum and Leishmania braziliensis. Furthermore, new simplified thiazolidenehydrazine derivatives were evaluated against Trypanosoma cruzi. The cytotoxicity of the active compounds on non-infected fibroblasts or macrophages was established in vitro to evaluate the selectivity of their anti-parasitic effects. Seven thiazolidenehydrazine derivatives and ten arylideneketones had good activity against the three parasites. The IC50 values for T. cruzi and Leishmania spp. ranged from 90 nM–25 μM. Eight compounds had multi-trypanocidal activity against T. cruzi and Leishmania spp. (the etiological agents of cutaneous and visceral forms). The selectivity of these active compounds was better than the three reference drugs: benznidazole, glucantime and miltefosine. They also had low toxicity when tested in vivo on zebrafish. Trying to understand the mechanism of action of these compounds, two possible molecular targets were investigated: triosephosphate isomerase and cruzipain. We also used a molecular stripping approach to elucidate the minimal structural requirements for their anti-T. cruzi activity.
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MDPI AG
EN:
Molecules, 2017, 22(5), art nº 709.
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Citación:
Álvarez, G, Perdomo, C, Coronel, C, [y otros autores]. "Multi-anti-parasitic activity of arylidene ketones and thiazolidene hydrazines against trypanosoma cruzi and Leishmania spp". Molecules. [en línea] 2017, 22(5), art nº 709. 26 h.
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ISSN:
1420-3049
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Licencia Creative Commons Atribución - No Comercial - Sin Derivadas (CC - By-NC-ND 4.0)
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| Ficheros | Descripción | Tamaño | Formato | ||
|---|---|---|---|---|---|
| 103390molecules22050709.pdf | — | 10.9 MB | Adobe PDF |