1,4-disubstituted thiosemicarbazide derivatives are potent inhibitors of toxoplasma gondii proliferation.
Data wydania
2014Autor
Dzitko, Katarzyna
Paneth, Agata
Plech, Tomasz
Pawełczyk, Jakub
Stączek, Paweł
Stefańska, Joanna
Paneth, Piotr
Metadata
Pokaż pełny rekordAbstrakt
A series of 4-arylthiosemicarbazides substituted at the N1 position with a
5-membered heteroaryl ring was synthesized and evaluated in vitro for T. gondii inhibition proliferation and host cell cytotoxicity. At non-toxic concentrations for the host cells all studied compounds displayed excellent anti-parasitic effects when compared to
sulfadiazine, indicating a high selectivity of their anti-T. gondii activity. The differences in
bioactivity investigated by DFT calculations suggest that the inhibitory activity of 4-arylthiosemicarbazides towards T. gondii proliferation is connected with the electronic
structure of the molecule. Further, these compounds were tested as potential antibacterial agents. No growth-inhibiting effect on any of the test microorganisms was observed for all the compounds, even at high concentrations.
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