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

Molecules

Katarzyna Dzitko⁵  Agata Paneth¹  Tomasz Plech¹  Jakub Paweᐬzyk⁴  Paweł Stၜzek²  Joanna Stefańska³ 

[1] Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland; E-Mails:;Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland; E-Mail:;Department of Pharmaceutical Microbiology, Medical University of Warsaw, Oczki 3, 02-007 Warszawa, Poland; E-Mail:;Institute for Medical Biology of the Polish Academy of Sciences, Lodowa 106, 93-232 Łódź, Poland; E-Mail:;Department of Immunoparasitology, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland

关键词: thiosemicarbazide derivatives;    anti-Toxoplasma gondii activity;    antibacterial activity;    bacterial topoisomerases;    toxicity;    docking studies;    DFT calculations;   

DOI  :  10.3390/molecules19079926

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.