title: Novel and promising compounds to treat Cryptosporidium parvum infections.
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.
authors.affiliation: W. Stefanski Institute of Parasitology, PAN, Warsaw, Poland.
authors.forename: Zofi
authors.initials: Z
authors.lastname: Graczyk
authors.forename: Lidia
authors.initials: L
authors.lastname: Chomicz
authors.forename: Mariola
authors.initials: M
authors.lastname: Kozłowska
authors.forename: Zygmunt
authors.initials: Z
authors.lastname: Kazimierczuk
authors.forename: Thaddeus K
authors.initials: TK
authors.lastname: Graczyk
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival; D016785:Cryptosporidium parvum / Q000187:drug effects* / Q000254:growth & development; D020895:Enterocytes / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D021261:Parasitic Sensitivity Tests
chemical_list: D000981:Antiprotozoal Agents; D001562:Benzimidazoles