Journal
MOLECULES
Volume 19, Issue 7, Pages 9926-9943Publisher
MDPI AG
DOI: 10.3390/molecules19079926
Keywords
thiosemicarbazide derivatives; anti-Toxoplasma gondii activity; antibacterial activity; bacterial topoisomerases; toxicity; docking studies; DFT calculations
Funding
- National Science Centre [2012/05/D/NZ7/02278]
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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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