Activity of imidazoles against Leishmania tropica in human macrophage cultures.
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 microgram/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.
D003022:Clotrimazole / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology* / Q000627:therapeutic use; D066298:In Vitro Techniques; D007654:Ketoconazole; D007891:Leishmania / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy; D008264:Macrophages / Q000469:parasitology*; D008825:Miconazole / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology
D007093:Imidazoles; D010879:Piperazines; D008825:Miconazole; D003022:Clotrimazole; D007654:Ketoconazole