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Bioorg Med Chem Lett. 2003 Nov 3;13(21):3783-7.

Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives.

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Institut de Biologie et Institut Pasteur de Lille, UMR 8525 CNRS, Université de Lille II, 1 rue du Professeur Calmette, B.P. 447, 59021 Lille, France.


Synthesis and evaluation of the activity of a new family of 1,4-bis(3-aminopropyl)piperazine derivatives against a chloroquine-resistant strain of Plasmodium falciparum, and as inhibitors of beta-hematin formation, are described. The highest antimalarial activities were obtained for compounds displaying the highest predicted vacuolar accumulation ratios and the best potencies as inhibitors of beta-hematin formation. The most potent compound displayed an activity 3-fold better than chloroquine for a comparable selectivity index upon MRC-5 cells. Therefore, in this series, the replacement of the 7-chloroquinoline group can constitute a strong rationale for further investigation.

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