Title of article :
Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening
Author/Authors :
Georgina A. Holloway، نويسنده , , Jonathan B. Baell، نويسنده , , Alan H. Fairlamb، نويسنده , , Patrizia M. Novello، نويسنده , , John P. Parisot، نويسنده , , John Richardson، نويسنده , , Keith G. Watson، نويسنده , , Ian P. Street، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2007
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.
Keywords :
Tropical diseases , Trypanosomiasis therapeutics , Trypanothione reductase inhibitors , High-throughput screening , medicinal chemistry , Iminobenzimidazoles
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters