Antitrypanosomal activity of fluoroquinolones

被引:39
作者
Nenortas, E [1 ]
Burri, C [1 ]
Sapiro, TA [1 ]
机构
[1] Johns Hopkins Univ, Sch Med, Dept Med, Div Clin Pharmacol, Baltimore, MD 21205 USA
关键词
D O I
10.1128/AAC.43.8.2066
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
Six fluoroquinolones presently in clinical use and four investigational tetracyclic fluoroquinolones were tested for in vitro activity against bloodstream-form Trypanosoma brucei brucei. All compounds had measurable activity, but the tetracyclic analogs were most potent, with 50% effective concentrations in the low micromolar range. In general, trypanosomes mere more susceptible than L1210 leukemia cells. Consistent with the notion that they target type II topoisomerase in trypanosomes, the fluoroquinolones promote the formation of protein-DNA covalent complexes.
引用
收藏
页码:2066 / 2068
页数:3
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