In-vitro and in-vivo activity of 1-hydroxy-2-alkyl-4(1H)quinolone derivatives against Toxoplasma

Antimicrob Agents Chemother. 2009 Nov 2. [Epub ahead of print]

In-vitro and in-vivo activity of 1-hydroxy-2-alkyl-4(1H)quinolone derivatives against Toxoplasma gondii

Bajohr LL, Ma L, Platte C, Liesenfeld O, Tietze LF, Groß U, Bohne W.

Institut für Mikrobiologie und Hygiene, Charité Universtätsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 27, 12203 Berlin, Germany; Institut für Organische und Biomolekulare Chemie, Universität Göttingen, Tammannstr. 2, D-37077 Göttingen, Germany; Institut für Medizinische Mikrobiologie, Universitätsmedizin Göttingen, Kreuzbergring 57, D-37075 Göttingen, Germany.

1-hydroxy-2-dodecyl-4(1)quinolone (HDQ) was recently identified as a Toxoplasma gondii inhibitor. We describe here two novel 1-hydroxyquinolones, which displayed a 10- and 5-fold lower IC50 than HDQ. In a mouse model of acute toxoplasmosis these two compounds and HDQ reduced the percentage of infected peritoneal cells and decreased the parasite load in lung and liver. Compound B showed a tendency towards lower parasite loads in brains in a mouse model of toxoplasmic encephalitis.

PMID: 19884369 [PubMed - as supplied by publisher]