Design, synthesis and antimalarial activity of a glyoxylylhydrazone library |
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| Authors: | Ryckebusch A Fruchart J-S Cattiaux L Rousselot-Paillet P Leroux V Melnyk O Grellier P Mouray E Sergheraert C Melnyk P |
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| Affiliation: | Institut de Biologie et Institut Pasteur de Lille--UMR CNRS 8525--Université de Lille II, 1 rue du Professeur Calmette, BP 447, 59021, France. |
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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. |
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