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

Agata PanethLidia WęglińskaAdrian BekierEdyta StefaniszynMonika WujecNazar TrotskoKatarzyna Dzitko
Published in: Molecules (Basel, Switzerland) (2019)
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.
Keyphrases
  • toxoplasma gondii
  • induced apoptosis
  • bioinformatics analysis
  • cell cycle arrest
  • high resolution
  • cell death
  • endoplasmic reticulum stress
  • oxidative stress
  • smoking cessation