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

作者：Holloway Georgina A; Baell Jonathan B; Fairlamb Alan H; Novello Patrizia M; Parisot John P; Richardson John; Watson Keith G; Street Ian P^*

来源：Bioorganic & Medicinal Chemistry Letters, 2007, 17(5): 1422-1427.

DOI：10.1016/j.bmcl.2006.11.090

• tropical diseases
• trypanosomiasis therapeutics
• trypanothione reductase inhibitors
• high-throughput screening
• medicinal chemistry
• iminobenzimidazoles

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.

• 出版日期2007-3-1
• 单位河北医科大学