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Molecules 2014, 19(7), 9926-9943; doi:10.3390/molecules19079926

1,4-Disubstituted Thiosemicarbazide Derivatives are Potent Inhibitors of Toxoplasma gondii Proliferation

1
Department of Immunoparasitology, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland
2
Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland
3
Institute of Applied Radiation Chemistry, Technical University of Lodz, Zeromskiego 116, 90-924 Lodz, Poland
4
Institute for Medical Biology of the Polish Academy of Sciences, Lodowa 106, 93-232 Łódź, Poland
5
Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland
6
Department of Pharmaceutical Microbiology, Medical University of Warsaw, Oczki 3, 02-007 Warszawa, Poland
*
Author to whom correspondence should be addressed.
Received: 11 June 2014 / Revised: 27 June 2014 / Accepted: 27 June 2014 / Published: 9 July 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [605 KB, uploaded 9 July 2014]   |  

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. View Full-Text
Keywords: thiosemicarbazide derivatives; anti-Toxoplasma gondii activity; antibacterial activity; bacterial topoisomerases; toxicity; docking studies; DFT calculations thiosemicarbazide derivatives; anti-Toxoplasma gondii activity; antibacterial activity; bacterial topoisomerases; toxicity; docking studies; DFT calculations
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Dzitko, K.; Paneth, A.; Plech, T.; Pawełczyk, J.; Stączek, P.; Stefańska, J.; Paneth, P. 1,4-Disubstituted Thiosemicarbazide Derivatives are Potent Inhibitors of Toxoplasma gondii Proliferation. Molecules 2014, 19, 9926-9943.

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