Artykuły (WCh)

Stały URI dla kolekcjihttp://hdl.handle.net/11652/155

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20141

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Autorsearch.filters.applied.operator.equals: search.filters.author.Paneth, PiotrTematsearch.filters.applied.operator.equals: search.filters.subject.bacterial topoisomerases

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  • Pozycja
    1,4-disubstituted thiosemicarbazide derivatives are potent inhibitors of toxoplasma gondii proliferation.
    (2014) Dzitko, Katarzyna; Paneth, Agata; Plech, Tomasz; Pawełczyk, Jakub; Stączek, Paweł; Stefańska, Joanna; Paneth, Piotr
    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.