Author/Authors :
A. Ryckebusch، نويسنده , , J.-S. Fruchart، نويسنده , , L. Cattiaux، نويسنده , , P. Rousselot-Paillet، نويسنده , , V. Leroux، نويسنده , , O. Melnyk، نويسنده , , P. Grellier، نويسنده , , E. Mouray، نويسنده , , C. Sergheraert، نويسنده , , P. Melnyk، نويسنده ,
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 β-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.
Keywords :
Antimalarial , Library.* Corresponding author. Tel.: +33-3-20-871219 , e-mail: patricia.melnyk@ibl.fr , fax: +33-3-20-871233 , Parallel synthesis , Glyoxylyl
