Systematic Identification of Thiosemicarbazides for Inhibition of <i>Toxoplasma gondii</i> 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 <i>Toxoplasma gondii</i>. In the search for such structures, thiosemicarbazide-based compounds have emerged as a nov...

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Bibliographic Details
Main Authors: Agata Paneth, Lidia Węglińska, Adrian Bekier, Edyta Stefaniszyn, Monika Wujec, Nazar Trotsko, Katarzyna Dzitko
Format: Article
Language:English
Published: MDPI AG 2019-02-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/24/3/614
Description
Summary: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 <i>Toxoplasma gondii</i>. 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-<i>Toxoplasma gondii</i> activity. The best 4-arylthiosemicarbazides <b>3</b> and <b>4</b> 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.
ISSN:1420-3049