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 were more susceptible than L1210 leukemia cells. Consistent with the notion that they target type H topoisomerase in trypanosomes, the fluoroquinolones promote the formation of protein-DNA covalent complexes.
|Original language||English (US)|
|Number of pages||3|
|Journal||Antimicrobial agents and chemotherapy|
|State||Published - Aug 1 1999|
ASJC Scopus subject areas
- Pharmacology (medical)
- Infectious Diseases