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  • Title: Design, synthesis and antimalarial activity of a glyoxylylhydrazone library.
    Author: Ryckebusch A, Fruchart JS, Cattiaux L, Rousselot-Paillet P, Leroux V, Melnyk O, Grellier P, Mouray E, Sergheraert C, Melnyk P.
    Journal: Bioorg Med Chem Lett; 2004 Sep 06; 14(17):4439-43. PubMed ID: 15357968.
    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.
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