Malaria continues to be an enormous health-threat in the developing world. Treatment is compounded by the phenomenon of drug resistance, and the development of novel therapeutics has become a research priority. Plasmodium falciparum (Pf) is the parasite responsible for the most dangerous form of human malaria, and the enzyme, 1-deoxy-1-D-xylulose 5-phosphate reductoisomerase (PfDXR) has recently been validated as a target for the design of potential antimalarial drugs.