Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening
- Author(s)
- Holloway, GA; Baell, JB; Fairlamb, AH; Novello, PM; Parisot, JP; Richardson, J; Watson, KG; Street, IP;
- Details
- Publication Year 2007-03-01,Volume 17,Issue #5,Page 1422-1427
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Publication Type
- Journal Article
- 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. (c) 2006 Elsevier Ltd. All rights reserved.
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- OXIDATIVE STRESS; ACTIVE-SITE; DRUG DESIGN; DERIVATIVES; TRYPANOSOMA; LEISHMANIA; CHEMOTHERAPY; BINDING; ASSAYS; GENE
- Publisher's Version
- https://doi.org/10.1016/j.bmcl.2006.11.090
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2007-03-01 12:00:00