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1,4-Disubstituted thiosemicarbazide derivatives are potent inhibitors of Toxoplasma gondii proliferation.

Authors
  • 1
  • 2
  • 3
  • 4
  • 5
  • 6
  • 7
  • 1 Department of Immunoparasitology, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland. [email protected] , (Poland)
  • 2 Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland. [email protected] , (Poland)
  • 3 Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland. [email protected] , (Poland)
  • 4 Institute for Medical Biology of the Polish Academy of Sciences, Lodowa 106, 93-232 Łódź, Poland. [email protected] , (Poland)
  • 5 Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland. [email protected] , (Poland)
  • 6 Department of Pharmaceutical Microbiology, Medical University of Warsaw, Oczki 3, 02-007 Warszawa, Poland. [email protected] , (Poland)
  • 7 Institute of Applied Radiation Chemistry, Technical University of Lodz, Zeromskiego 116, 90-924 Lodz, Poland. [email protected] , (Poland)
Type
Published Article
Journal
Molecules
1420-3049
Publisher
MDPI AG
Publication Date
Volume
19
Issue
7
Pages
9926–9943
Identifiers
DOI: 10.3390/molecules19079926
PMID: 25010466
Source
Medline
License
Unknown

Abstract

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-aryl-thiosemicarbazides 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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