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Discovery of nitroheterocycles active against African trypanosomes. in vitro screening and preliminary SAR studies

AuthorsArán, Vicente J. ; Kaiser, M.; Dardonville, Christophe
Issue Date2012
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry Letters 22: 4506- 4516 (2012)
AbstractA selection of 76 nitroheterocycles and related compounds from our in-house compound library was screened in vitro against the parasite Trypanosoma brucei rhodesiense, causative agent of human African trypanosomiasis (HAT). The unspecific cytotoxicity of the compounds was also evaluated against rat myoblast L6-cells to measure the selectivity of the compounds towards the parasite. This screening revealed some preliminary structure-activity relationships (SAR) among the series, and six hit compounds showing interesting activity (IC 50 ≤10 μM) and fair selectivity (SI >17). The 7-nitroquinoxalin-2-one and 5-nitroindazole scaffold derivatives 58 and 35, respectively, are particularly interesting because of their established oral bioavailability in mice. These hits represent interesting starting points for a medicinal project aimed at identifying the SAR behind this class of compounds. © 2012 Elsevier Ltd. All rights reserved.
Publisher version (URL)http://dx.doi.org/10.1016/j.bmcl.2012.06.004
Identifiersdoi: 10.1016/j.bmcl.2012.06.004
issn: 0960-894X
e-issn: 1464-3405
Appears in Collections:(IQM) Artículos
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