title: Quinonic derivatives active against Toxoplasma gondii.
abstract: Quinonic derivatives were tested against a virulent RH strain of Toxoplasma gondii maintained in cell culture in THP-1, a human myelomonocytic cell line. The derivatives were tested at various doses (0.5-4 microg/ml) and compared with the reference molecules clindamycine, sulfadiazine, pyrimethamine and atovaquone. The percentage of parasite growth inhibition was observed after 72 h of incubation. The tested derivatives are bicyclic, tricyclic or tetracyclic quinones. Eight of these compounds exhibit over 70% inhibition of parasite growth; and two were nearly equipotent to pyrimethamine. These data indicate that the most active compounds against the RH strain of T. gondii are bis-heterocyclic quinones.
authors.affiliation: Department of Parasitology and Medical Mycology, EA 1887, Claude Bernard University, 8 avenue Rockefeller, 69373 Lyon Cedex, France. sarciron@cismsun.univ-lyon1.fr
authors.forename: Marie-Elisabeth
authors.initials: ME
authors.lastname: Sarciron
authors.forename: Pascal
authors.initials: P
authors.lastname: Nebois
authors.forename: Félix
authors.initials: F
authors.lastname: Pautet
authors.forename: Anne-Françoise
authors.initials: AF
authors.lastname: Pétavy
authors.forename: Houda
authors.initials: H
authors.lastname: Fillion
authors.forename: Nadia
authors.initials: N
authors.lastname: Walchshofer
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D020128:Inhibitory Concentration 50; D021261:Parasitic Sensitivity Tests / Q000379:methods; D011809:Quinones / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014122:Toxoplasma / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000981:Antiprotozoal Agents; D011809:Quinones