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

…, JP Parisot, J Richardson, KG Watson, IP Street

Index: Holloway, Georgina A.; Baell, Jonathan B.; Fairlamb, Alan H.; Novello, Patrizia M.; Parisot, John P.; Richardson, John; Watson, Keith G.; Street, Ian P. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1422 - 1427

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Citation Number: 45

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.