Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 14, Pages 3835-3839Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.04.088
Keywords
Trypanosoma cruzi; growth inhibitors; anti-parasitic agents
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Quinoxaline derivatives presented good inhibitor activity of growth of Trypanosoma cruzi in in vitro assays. The 50% inhibitory doses were of the same order of that of Nifurtimox. Derivative 13, a quinoxaline N,N'-dioxide derivative, and the reduced derivatives 19 and 20 were the most cytotoxic compounds against the protozoan. Structural requirements for optimal activity were studied by computational methods. From statistical analysis we could establish a multiple correlation between activity and lipophilic properties and LUMO energy. (C) 2004 Elsevier Ltd. All rights reserved.
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