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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

Research output: Contribution to journalArticleResearchpeer-review

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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