Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines

…, S Girault, L Maes, MA Debreu-Fontaine…

Index: Delarue; Girault; Maes; Debreu-Fontaine; Labaeid; Grellier; Sergheraert Journal of Medicinal Chemistry, 2001 , vol. 44, # 17 p. 2827 - 2833

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Citation Number: 58

Abstract

A new series of 4-anilinoquinolines with two proton-accepting side chains has been synthesized. Antimalarial activity and levels of cytotoxicity upon both MRC-5 cells and macrophages were found to be highly dependent upon the features of these side chains. Several compounds were found to be active in the low nanomolar range, against both chloroquine-sensitive and-resistant strains of Plasmodium falciparum in vitro. From among ...