caa a22 4500 445340150 CHVBK 20180317142809.0 cr unu---uuuuu 170323e20110901xx s 000 0 eng 10.1007/s00436-011-2290-y doi (NATIONALLICENCE)springer-10.1007/s00436-011-2290-y Novel and promising compounds to treat Cryptosporidium parvum infections [Elektronische Daten] [Zofi Graczyk, Lidia Chomicz, Mariola Kozłowska, Zygmunt Kazimierczuk, Thaddeus Graczyk] 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 (IC50 28-31μM). 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. The Author(s), 2011 Graczyk Zofi W. Stefanski Institute of Parasitology, PAN, Warsaw, Poland aut Chomicz Lidia Department of Medical Biology, Medical University of Warsaw, Warsaw, Poland aut Kozłowska Mariola Institute of Chemistry, Warsaw University of Life Sciences, Warsaw, Poland aut Kazimierczuk Zygmunt Institute of Chemistry, Warsaw University of Life Sciences, Warsaw, Poland aut Graczyk Thaddeus Department of Environmental Health Sciences, Johns Hopkins Bloomberg School of Public Health, Baltimore, MD, USA aut Parasitology Research Springer-Verlag 109/3(2011-09-01), 591-594 0932-0113 109:3<591 2011 109 436 https://doi.org/10.1007/s00436-011-2290-y text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s00436-011-2290-y text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Graczyk Zofi W. Stefanski Institute of Parasitology, PAN, Warsaw, Poland aut NATIONALLICENCE 700 1- Chomicz Lidia Department of Medical Biology, Medical University of Warsaw, Warsaw, Poland aut NATIONALLICENCE 700 1- Kozłowska Mariola Institute of Chemistry, Warsaw University of Life Sciences, Warsaw, Poland aut NATIONALLICENCE 700 1- Kazimierczuk Zygmunt Institute of Chemistry, Warsaw University of Life Sciences, Warsaw, Poland aut NATIONALLICENCE 700 1- Graczyk Thaddeus Department of Environmental Health Sciences, Johns Hopkins Bloomberg School of Public Health, Baltimore, MD, USA aut NATIONALLICENCE 773 0- Parasitology Research Springer-Verlag 109/3(2011-09-01), 591-594 0932-0113 109:3<591 2011 109 436 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer