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Molecules 2019, 24(3), 614; https://doi.org/10.3390/molecules24030614

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

1
Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland
2
Department of Immunoparasitology, Faculty of Biology and Environmental Protection, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland
*
Authors to whom correspondence should be addressed.
Received: 22 January 2019 / Revised: 5 February 2019 / Accepted: 7 February 2019 / Published: 10 February 2019
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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. View Full-Text
Keywords: thiosemicarbazides; anti-Toxoplasma gondii activity; toxicity; SAR analysis thiosemicarbazides; anti-Toxoplasma gondii activity; toxicity; SAR analysis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Paneth, A.; Węglińska, L.; Bekier, A.; Stefaniszyn, E.; Wujec, M.; Trotsko, N.; Dzitko, K. Systematic Identification of Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro. Molecules 2019, 24, 614.

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