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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 (IC 50s 10.30-113.45 µg/mL vs. ~2721.45 µg/mL). The most potent of them, 12, 13, and 15, blocked the in vitro proliferation of T. gondii more potently than trimethoprim (IC 50 12.13 µg/mL), as well. The results of lipophilicity studies collectively suggest that log P would be a rate-limiting factor for the anti- Toxoplasma activity of this class of compounds.

molecules/molecules online/molecules annual

Discovery of Potent and Selective Halogen-Substituted Imidazole-Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro via Structure-Based Design