MECHANISM-BASED DESIGN OF PARASITE-TARGETED ARTEMISININ DERIVATIVES -SYNTHESIS AND ANTIMALARIAL ACTIVITY OF BENZYLAMINO AND ALKYLAMINO ETHER ANALOGS OF ARTEMISININ

Several artemisinin derivatives linked to benzylamino and alkylamino g roups were synthesized in order to enhance accumulation within the mal aria parasite. The in vitro antimalarial activity was assessed against the chloroquine sensitive HB3 strain and the chloroquine resistant K1 strain of Plasmodium falciparum. In general the incorporation of amin o functionality enhances the activity relative to artemisinin. The mos t potent analogue in the series was compound 6 which was severalfold m ore active than artemisinin against both strains of P. falciparum used in the study.