306954-97-2Relevant academic research and scientific papers
1,4-disubstituted thiosemicarbazide derivatives are potent inhibitors of toxoplasma gondii proliferation
Dzitko, Katarzyna,Paneth, Agata,Plech, Tomasz,Pawelczyk, Jakub,Staczek, Pawel,Stefanska, Joanna,Paneth, Piotr
, p. 9926 - 9943 (2014/08/05)
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.
