Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1399832 | European Journal of Medicinal Chemistry | 2008 | 9 Pages |
Abstract
In order to determine the real significance of the 4′-phenolic group in the antimalarial activity and/or cytotoxicity of amodiaquine (AQ), analogues for which this functionality was shifted or modified were synthesized. Good in vitro antimalarial activity was obtained for compounds unable to form intramolecular hydrogen bond. Among the compounds synthesized, new amino derivative 5 displayed the greatest selectivity index towards the most CQ-resistant strain tested and was active in mice infected by Plasmodium berghei.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sandrine Delarue-Cochin, Emilia Paunescu, Louis Maes, Elisabeth Mouray, Christian Sergheraert, Philippe Grellier, Patricia Melnyk,