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

Georgina A. Holloway, Jonathan B. Baell, Alan H. Fairlamb, Patrizia M. Novello, John P. Parisot, John Richardson, Keith G. Watson, Ian P. Street (Lead / Corresponding author)

    Research output: Contribution to journalArticlepeer-review

    47 Citations (Scopus)

    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.

    Original languageEnglish
    Pages (from-to)1422-1427
    Number of pages6
    JournalBioorganic and Medicinal Chemistry Letters
    Volume17
    Issue number5
    DOIs
    Publication statusPublished - 1 Mar 2007

    Keywords

    • High-throughput screening
    • Iminobenzimidazoles
    • Medicinal chemistry
    • Tropical diseases
    • Trypanosomiasis therapeutics
    • Trypanothione reductase inhibitors

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