title: Triazole-based compound as a candidate to develop novel medicines to treat toxoplasmosis.
abstract: This article reports anti-Toxoplasma gondii activity of 3-(thiophen-2-yl)-1,2,4-triazole-5-thione. The compound displayed significant and reproducible antiparasitic effects at nontoxic concentrations for the host cells, with an experimentally determined 50% inhibitory concentration (IC50) at least 30 times better than that of the known chemotherapeutic agent sulfadiazine. Purine nucleoside phosphorylase was defined as the probable target for anti-Toxoplasma activity of the tested compound. These results provide the foundation for future work to develop a new class of medicines to better treat toxoplasmosis.
authors.affiliation: Department of Immunoparasitology, University of Lodz, Lodz, Poland dzika@biol.uni.lodz.pl.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Dzitko
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Lublin, Poland Institute of Applied Radiation Chemistry, Technical University of Lodz, Poland.
authors.forename: Agata
authors.initials: A
authors.lastname: Paneth
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Lublin, Poland.
authors.forename: Tomasz
authors.initials: T
authors.lastname: Plech
authors.affiliation: Institute for Medical Biology of the Polish Academy of Sciences, Lodz, Poland.
authors.forename: Jakub
authors.initials: J
authors.lastname: Pawełczyk
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Lublin, Poland.
authors.forename: Lidia
authors.initials: L
authors.lastname: Węglińska
authors.affiliation: Institute of Applied Radiation Chemistry, Technical University of Lodz, Poland.
authors.forename: Piotr
authors.initials: P
authors.lastname: Paneth
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D005347:Fibroblasts / Q000187:drug effects / Q000469:parasitology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D062105:Molecular Docking Simulation; D021261:Parasitic Sensitivity Tests; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011683:Purine-Nucleoside Phosphorylase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D013411:Sulfadiazine / Q000494:pharmacology; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014122:Toxoplasma / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C000599189:3-(thiophen-2-yl)-1,2,4-triazole-5-thione; D000981:Antiprotozoal Agents; D015800:Protozoan Proteins; D013876:Thiophenes; D014230:Triazoles; D013411:Sulfadiazine; D011683:Purine-Nucleoside Phosphorylase