Journal
MOLECULES
Volume 24, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules24081618
Keywords
thiosemicarbazides; anti-Toxoplasma gondii activity; cytotoxicity; selectivity ratio; structure-activity relationship (SAR) analysis
Funding
- Medical University of Lublin [DS 15]
- Faculty of Biology and Environmental Protection, University of Lodz [B1711000000263.01]
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Employing a simple synthetic protocol, a series of highly effective halogen-substituted imidazole-thiosemicarbazides with anti-Toxoplasma gondii effects against the RH tachyzoites, much better than sulfadiazine, were obtained (IC50s 10.30113.45 mu g/mL vs. 2721.45 mu g/mL). The most potent of them, 12, 13, and 15, blocked the in vitro proliferation of T. gondii more potently than trimethoprim (IC50 12.13 mu g/mL), as well. The results of lipophilicity studies collectively suggest that logP would be a rate-limiting factor for the anti-Toxoplasma activity of this class of compounds.
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