1. Novel and promising compounds to treat Cryptosporidium parvum infections.
- Author
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Graczyk Z, Chomicz L, Kozłowska M, Kazimierczuk Z, and Graczyk TK
- Subjects
- Animals, Antiprotozoal Agents chemistry, Benzimidazoles chemistry, Cell Line, Cell Survival, Cryptosporidium parvum growth & development, Enterocytes parasitology, Humans, Inhibitory Concentration 50, Parasitic Sensitivity Tests, Antiprotozoal Agents pharmacology, Benzimidazoles pharmacology, Cryptosporidium parvum drug effects
- Abstract
No fully effective approved drug therapy exists for Cryptosporidium infections of immunocompetent and immunocompromised patients. Here, we investigated 11 benzimidazole derivatives carrying substituted thioalkyl and thiobenzyl groups at position 2 of benzimidazole nucleus and additional substituents at the benzene part of benzimidazole for inhibition of the in vitro growth of the intestinal protozoan parasite, Cryptosporidium parvum. Three of them, i.e., 5-carboxy-2-(4-nitrobenzylthio)-1H-benzimidazole, 5,6-dichloro-2-(4-nitrobenzylthio)-1H-benzimidazole, and 4,6-dichloro-2-(4-nitrobenzylthio)-1H-benzimidazole, (compounds 5, 7, and 8) were the most active (IC(50) 28-31 μM). The concentration of compounds 5, 7, and 8 that caused 50% growth inhibition in human enterocytic HCT-8 cells by a quantitative alkaline phosphatase immunoassay was comparable with those obtained for paromomycin.
- Published
- 2011
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