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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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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
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author Paneth, Agata
Węglińska, Lidia
Bekier, Adrian
Stefaniszyn, Edyta
Wujec, Monika
Trotsko, Nazar
Dzitko, Katarzyna
author_facet Paneth, Agata
Węglińska, Lidia
Bekier, Adrian
Stefaniszyn, Edyta
Wujec, Monika
Trotsko, Nazar
Dzitko, Katarzyna
author_sort Paneth, Agata
collection PubMed
description 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.
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spelling pubmed-63847302019-02-23 Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro Paneth, Agata Węglińska, Lidia Bekier, Adrian Stefaniszyn, Edyta Wujec, Monika Trotsko, Nazar Dzitko, Katarzyna Molecules Article 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. MDPI 2019-02-10 /pmc/articles/PMC6384730/ /pubmed/30744161 http://dx.doi.org/10.3390/molecules24030614 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Paneth, Agata
Węglińska, Lidia
Bekier, Adrian
Stefaniszyn, Edyta
Wujec, Monika
Trotsko, Nazar
Dzitko, Katarzyna
Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro
title Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro
title_full Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro
title_fullStr Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro
title_full_unstemmed Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro
title_short Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro
title_sort systematic identification of thiosemicarbazides for inhibition of toxoplasma gondii growth in vitro
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6384730/
https://www.ncbi.nlm.nih.gov/pubmed/30744161
http://dx.doi.org/10.3390/molecules24030614
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