Bioorg Med Chem Lett. 2007 Mar 1;17(5):1422-7. Epub 2006 Dec 3.

Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening.

Holloway GA, Baell JB, Fairlamb AH, Novello PM, Parisot JP, Richardson J, Watson KG, Street IP.

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The Walter and Eliza Hall Institute of Medical Research, Biotechnology Centre, 4 Research Avenue, La Trobe Research and Development Park, Bundoora, Vic. 3086, Australia.

Abstract

A high-throughput screening campaign of a library of 100,000 lead-like compounds identified 2-iminobenzimidazoles as a novel class of trypanothione reductase inhibitors. These 2-iminobenzimidazoles display potent trypanocidal activity against Trypanosoma brucei rhodesiense, do not inhibit closely related human glutathione reductase and have low cytotoxicity against mammalian cells.

PMID:: 17194585; [PubMed - indexed for MEDLINE]

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Research Support, Non-U.S. Gov't

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079838/Wellcome Trust/United Kingdom

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Cited by 9 PubMed Central articles

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography. [J Med Chem. 2011]
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