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Am. J. Trop. Med. Hyg., 30(3), 1981, pp. 566-569
Copyright © 1981 by The American Society of Tropical Medicine and Hygiene

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Activity of Imidazoles Against Leishmania Tropica in Human Macrophage Cultures*

Jonathan Dembitz Berman
Cell Biology Section, Laboratory of Parasitic Diseases, National Institutes of Health, Bethesda, Maryland 20205, and Department of Parasitology, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, D.C. 20012

The anti-leishmanial activity of four imidazoles has been determined in Leishmania tropica-infected human monocyte-derived macrophage cultures. One of the imidazoles, hydrolyzed ketoconazole [cis-1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxyphenyl}piperazine], eliminated 80 and 95% of the parasites at drug concentrations (2.0 and 2.5 µg/ml) that are achievable in vivo by a structurally similar compound, ketoconazole. These results demonstrate that an imidazole has anti-leishmanial activity in a model system, and suggests that hydrolyzed ketoconazole should be considered for in vivo trials in animal models of the disease.

Accepted for publication December 13, 1980.


* Address reprint requests to: Dr. Jonathan D. Berman, Division of Experimental Therapeutics, Department of Parasitology, Walter Reed Army Institute of Research, Washington, D.C. 20012.




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Copyright © 1981 by the American Society of Tropical Medicine and Hygiene.