In vitro and in vivo activities of 1-hydroxy-2-alkyl-4(1H)quinolone derivatives against Toxoplasma gondii.
1-Hydroxy-2-dodecyl-4(1H)quinolone (HDQ) was recently identified as a Toxoplasma gondii inhibitor. We describe here two novel 1-hydroxyquinolones, which displayed 50% inhibitory concentrations 10- and 5-fold lower than that of HDQ. In a mouse model of acute toxoplasmosis, these two compounds and HDQ reduced the percentages of infected peritoneal cells and decreased the parasite loads in lungs and livers. Compound B showed a tendency toward lowering parasite loads in brains in a mouse model of toxoplasmic encephalitis.
Bajohr
Lara Liv
LL
Institut für Mikrobiologie und Hygiene, Charité Universtätsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 27, 12203 Berlin, Germany.
Ma
Ling
L
Platte
Christian
C
Liesenfeld
Oliver
O
Tietze
Lutz F
LF
Gross
Uwe
U
Bohne
Wolfgang
W
D000818:Animals; D000977:Antiparasitic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002478:Cells, Cultured; D016054:DNA, Protozoan / Q000032:analysis; D005260:Female; D005347:Fibroblasts / Q000187:drug effects / Q000469:parasitology; D005434:Flow Cytometry; D006801:Humans; D008099:Liver / Q000737:chemistry / Q000469:parasitology; D008168:Lung / Q000737:chemistry / Q000469:parasitology; D051379:Mice; D010529:Peritoneal Cavity / Q000166:cytology / Q000469:parasitology; D015363:Quinolones / Q000494:pharmacology* / Q000627:therapeutic use; D020133:Reverse Transcriptase Polymerase Chain Reaction; D014122:Toxoplasma / Q000187:drug effects*; D014124:Toxoplasmosis, Animal / Q000188:drug therapy* / Q000469:parasitology; D016781:Toxoplasmosis, Cerebral / Q000188:drug therapy / Q000469:parasitology
D000977:Antiparasitic Agents; D016054:DNA, Protozoan; D015363:Quinolones