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Antimicrobial Agents and Chemotherapy, August 1999, p. 2066-2068, Vol. 43, No. 8
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

Antitrypanosomal Activity of Fluoroquinolones

Elizabeth Nenortas, Christian Burri,dagger and Theresa A. Shapiro*

Division of Clinical Pharmacology, Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205-2185

Received 9 March 1999/Returned for modification 4 May 1999/Accepted 27 May 1999

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 II topoisomerase in trypanosomes, the fluoroquinolones promote the formation of protein-DNA covalent complexes.

* Corresponding author. Mailing address: Division of Clinical Pharmacology, Department of Medicine, Johns Hopkins University School of Medicine, 301 Hunterian Building, 725 North Wolfe St., Baltimore, MD 21205-2185. Phone: (410) 955-1888. Fax: (410) 955-2634.

dagger Present address: Swiss Tropical Institute, Department of Medical Parasitology and Infection Biology, 4002 Basel, Switzerland.

Antimicrobial Agents and Chemotherapy, August 1999, p. 2066-2068, Vol. 43, No. 8
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.


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