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Bioorg Med Chem Lett. 2012 Mar 1;22(5):1985-8. doi: 10.1016/j.bmcl.2012.01.029. Epub 2012 Jan 24.

Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.

Author information

1
Department of Biology, Brandeis University, MS009, 415 South Street, Waltham, MA 02454, USA.

Abstract

Cryptosporidium parasites are important waterborne pathogens of both humans and animals. The Cryptosporidium parvum and Cryptosporidium hominis genomes indicate that the only route to guanine nucleotides is via inosine 5'-monophosphate dehydrogenase (IMPDH). Thus the inhibition of the parasite IMPDH presents a potential strategy for treating Cryptosporidium infections. A selective benzimidazole-based inhibitor of C. parvum IMPDH (CpIMPDH) was previously identified in a high throughput screen. Here we report a structure-activity relationship study of benzimidazole-based compounds that resulted in potent and selective inhibitors of CpIMPDH. Several compounds display potent antiparasitic activity in vitro.

PMID:
22310229
PMCID:
PMC3289519
DOI:
10.1016/j.bmcl.2012.01.029
[Indexed for MEDLINE]
Free PMC Article

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