1,4-disubstituted thiosemicarbazide derivatives are potent inhibitors of toxoplasma gondii proliferation.
| dc.contributor.author | Dzitko, Katarzyna | |
| dc.contributor.author | Paneth, Agata | |
| dc.contributor.author | Plech, Tomasz | |
| dc.contributor.author | Pawełczyk, Jakub | |
| dc.contributor.author | Stączek, Paweł | |
| dc.contributor.author | Stefańska, Joanna | |
| dc.contributor.author | Paneth, Piotr | |
| dc.date.accessioned | 2016-01-29T07:44:51Z | |
| dc.date.available | 2016-01-29T07:44:51Z | |
| dc.date.issued | 2014 | |
| dc.description.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-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. | pl_PL |
| dc.identifier.citation | Molecules 2014, 19, p. 9926-9943 | en_EN |
| dc.identifier.issn | 1420-3049 | |
| dc.identifier.uri | http://hdl.handle.net/11652/1002 | |
| dc.identifier.uri | http://www.mdpi.com/1420-3049/19/7/9926 | |
| dc.language.iso | en_EN | en_EN |
| dc.relation.ispartofseries | Molecules 2014, 19 | |
| dc.subject | thiosemicarbazide derivatives | en_EN |
| dc.subject | anti-Toxoplasma gondii activity | en_En |
| dc.subject | antibacterial activity | en_EN |
| dc.subject | bacterial topoisomerases | en_En |
| dc.subject | toxicity | en_EN |
| dc.subject | docking studies | en_EN |
| dc.subject | DFT calculations | en_EN |
| dc.title | 1,4-disubstituted thiosemicarbazide derivatives are potent inhibitors of toxoplasma gondii proliferation. | en_EN |
| dc.type | Artykuł | pl_PL |
| dc.type | Article | en_EN |