Quinonic derivatives active against Toxoplasma gondii.
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.
Sarciron
Marie-Elisabeth
ME
Department of Parasitology and Medical Mycology, EA 1887, Claude Bernard University, 8 avenue Rockefeller, 69373 Lyon Cedex, France. sarciron@cismsun.univ-lyon1.fr
Nebois
Pascal
P
Pautet
Félix
F
Pétavy
Anne-Françoise
AF
Fillion
Houda
H
Walchshofer
Nadia
N
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
D000981:Antiprotozoal Agents; D011809:Quinones