In Vitro and In Vivo Activities of 1-Hydroxy-2-Alkyl-4(1H)Quinolone Derivatives against Toxoplasma gondii
In Vitro and In Vivo Activities of 1-Hydroxy-2-Alkyl-4(1H)Quinolone Derivatives against Toxoplasma gondii
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DOI：
10.1128/aac.01001-09
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发表时间：
2010-01-01
影响因子：
4.9
通讯作者：
Bohne, Wolfgang
中科院分区：
文献类型：
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作者：
Bajohr, Lara Liv;Ma, Ling;Bohne, Wolfgang
1-羟基-2-十二烷基-4（1H）喹诺酮（HDQ）最近被发现是一种弓形虫抑制剂。我们在这里描述了两种新的1-羟基喹诺酮类药物，它们显示50%的抑制浓度比HDQ低10倍和5倍。在急性弓形虫病小鼠模型中，这两种化合物和HDQ降低了感染腹膜细胞的百分比，并降低了肺和肝脏中的寄生虫负荷。化合物B在弓形虫脑炎小鼠模型中显示出降低脑内寄生虫负荷的趋势。
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.