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Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro

One of the key stages in the development of new therapies in the treatment of toxoplasmosis is the identification of new non-toxic small molecules with high specificity to Toxoplasma gondii. In the search for such structures, thiosemicarbazide-based compounds have emerged as a novel and promising le...

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Detalles Bibliográficos
Autores principales: Paneth, Agata, Węglińska, Lidia, Bekier, Adrian, Stefaniszyn, Edyta, Wujec, Monika, Trotsko, Nazar, Dzitko, Katarzyna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6384730/
https://www.ncbi.nlm.nih.gov/pubmed/30744161
http://dx.doi.org/10.3390/molecules24030614
Descripción
Sumario:One of the key stages in the development of new therapies in the treatment of toxoplasmosis is the identification of new non-toxic small molecules with high specificity to Toxoplasma gondii. In the search for such structures, thiosemicarbazide-based compounds have emerged as a novel and promising leads. Here, a series of imidazole-thiosemicarbazides with suitable properties for CNS penetration was evaluated to determine the structural requirements needed for potent anti-Toxoplasma gondii activity. The best 4-arylthiosemicarbazides 3 and 4 showed much higher potency when compared to sulfadiazine at concentrations that are non-toxic to the host cells, indicating a high selectivity of their anti-toxoplasma activity.