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

Georgina A Holloway, Jonathan Bayldon Baell, Alan H Fairlamb, Patrizia M Novello, John P Parisot, John Richardson, Keith Geoffrey Watson, Ian Philip Street

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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 - 2007
Externally publishedYes

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