@article{f951a9878cde46fcaac94c764d719f8c,
title = "Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening",
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 = "High-throughput screening, Iminobenzimidazoles, Medicinal chemistry, Tropical diseases, Trypanosomiasis therapeutics, Trypanothione reductase inhibitors",
author = "Holloway, {Georgina A.} and Baell, {Jonathan B.} and Fairlamb, {Alan H.} and Novello, {Patrizia M.} and Parisot, {John P.} and John Richardson and Watson, {Keith G.} and Street, {Ian P.}",
note = "Funding Information: This investigation received financial support from the UNICEF/UNDP/World Bank/WHO special program for research and training in tropical diseases (TDR). We gratefully acknowledge Bill Charman, the center for drug candidate optimization (CDCO), for advice, valuable discussion and encouragement. We also express our gratitude for the support of the TDR screening network, in particular Reto Brun and his group at the Swiss tropical institute for conducting the anti-trypanosomal and cytoxicity assays. We also acknowledge Ahilan Saravanamuthu for conducting the early TR assay development.",
year = "2007",
month = mar,
day = "1",
doi = "10.1016/j.bmcl.2006.11.090",
language = "English",
volume = "17",
pages = "1422--1427",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier",
number = "5",
}
