New malaria drugs arise from the old

Novel derivatives of artemisinin, the active compound in an ancient Chinese remedy for malaria, could be just what the doctor ordered in the hunt for innovative treatments for drug-resistant malaria. Several new compounds, including the one shown, cure the disease in mice with just one to three doses, according to Gary H. Posner and colleagues at Johns Hopkins University (J. Med. Chem., DOI: 10.1021/jm070149m). Artemisinin derivatives already in use to treat malaria require higher doses. And unlike the new compounds, the older versions must be combined with other drugs. Both of those factors have limited the affordability of artemisinin-based treatments in developing nations. The new compounds were designed to be more stable and lipophilic than previous derivatives in order to improve efficacy, and they are among the most promising of nearly 1,000 antimalarial compounds that Posner's group has designed and evaluated during the past 15 years. The group is collaborating with a pharmaceutical company to further test and develop the compounds.