Antimalarial Substances

The malaria organism Plasmodium falciparum detoxifies heme, which is released upon degradation of host erythrocyte hemoglobin, by sequestering it within the parasite digestive vacuole in the form of a polymer called hemozoin. The antimalarial agent Chloroquine® acts by interrupting heme polymerization, yet its efficacy is impaired by drug-resistant organisms. The synthetic complex ethylenediamine-N,N'-bis[propyl(2-hydroxy-(R)-benzylimino)]alumi-num(III) (Figure 4.4) kills intraerythrocytic malaria parasites in a stage-specific manner, thus reflecting a new class of probes for Chloroquine®-resistant mechanisms and a fresh prospect in antimalarial drug development.59

Figure 4.4 The Schiff-base reduced amino derivative ligand used for the synthesis of the proposed octahedral (R)-ENBPA-Al(III) complex

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