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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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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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. |
format | Online Article Text |
id | pubmed-6384730 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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