4.6 Article

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

Journal

MOLECULES
Volume 24, Issue 3, Pages -

Publisher

MDPI
DOI: 10.3390/molecules24030614

Keywords

thiosemicarbazides; anti-Toxoplasma gondii activity; toxicity; SAR analysis

Funding

  1. Medical University of Lublin [DS 15]
  2. Faculty of Biology and Environmental Protection, University of Lodz [B1711000000263.01]

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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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