Details

Autor(en) / Beteiligte

• Paneth, Agata
• Węglińska, Lidia
• Bekier, Adrian
• Stefaniszyn, Edyta
• Wujec, Monika
• Trotsko, Nazar
• Hawrył, Anna
• Hawrył, Miroslaw
• Dzitko, Katarzyna

Titel

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

Ist Teil von

• Molecules (Basel, Switzerland), 2019-04, Vol.24 (8), p.1618

Ort / Verlag

Switzerland: MDPI AG

Erscheinungsjahr

2019

Link zum Volltext

Quelle

EZB Free E-Journals

Beschreibungen/Notizen

• Employing a simple synthetic protocol, a series of highly effective halogen-substituted imidazole-thiosemicarbazides with anti- effects against the RH tachyzoites, much better than sulfadiazine, were obtained (IC 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 more potently than trimethoprim (IC 12.13 µg/mL), as well. The results of lipophilicity studies collectively suggest that log would be a rate-limiting factor for the anti- activity of this class of compounds.