Published in
Elsevier, Bioorganic and Medicinal Chemistry Letters, 17(14), p. 4439-4443, 2004
DOI: 10.1016/j.bmcl.2004.06.056
Wiley-VCH Verlag, ChemInform, 51(35), 2004
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Design, Synthesis and Antimalarial Activity of a Glyoxylylhydrazone Library.
,
P. Rousselot-Paillet,
V. Leroux,
O. Melnyk ,
P. Grellier,
E. Mouray,
C. Sergheraert,
P. Melnyk
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Abstract
Synthesis of a new family of quinolylhydrazone derivatives and evaluation of their activity against a chloroquine-resistant strain of Plasmodium falciparum are described. The best compound displayed an activity 6-fold higher than chloroquine. None of the active compounds were found to inhibit beta-hematin formation in vitro in the same range as chloroquine and five among them displayed lower calculated vacuolar accumulation ratios, suggesting the implication of a different mechanism of action.