Design and synthesis of new antimalarial agents from 4-aminoquinoline

This study describes the synthesis of new 4-aminoquinoline derivatives and evaluation of their activity against a chloroquine sensitive strain of P. falciparum in vitro and chloroquine resistant N-67 strain of P. yoelii in vivo. All the analogues were found to form strong complex with hematin and inhibit the P-hematin formation in vitro. These results suggest that these compounds act on heme polymerization target. (c) 2005 Elsevier Ltd. All rights reserved.