New Antimalarial Drugs

• Published in: Angewandte Chemie International Edition 2003-11, Vol.42 (43), p.5274-5293
• Main Authors: Wiesner, Jochen, Ortmann, Regina, Jomaa, Hassan, Schlitzer, Martin
• Format: Article
• Language: English
• Subjects: Aminoquinolines - pharmacology; Aminoquinolines - therapeutic use; Animals; Antimalarials - pharmacology; Antimalarials - therapeutic use; Artemisinins - pharmacology; Artemisinins - therapeutic use; Atovaquone; biological targets; Clinical Trials as Topic; Dapsone - pharmacology; Dapsone - therapeutic use; Drug Combinations; Drug Design; Drug Resistance - genetics; Ethanolamines - pharmacology; Ethanolamines - urine; Flavonoids - pharmacology; Flavonoids - therapeutic use; Fluorenes - pharmacology; Fluorenes - urine; Fosfomycin - analogs & derivatives; Fosfomycin - pharmacology; Fosfomycin - therapeutic use; Global Health; Humans; malaria; Malaria - drug therapy; Malaria - epidemiology; Malaria - prevention & control; medicinal chemistry; Naphthoquinones - pharmacology; Naphthoquinones - therapeutic use; Naphthyridines - pharmacology; Naphthyridines - therapeutic use; Plasmodium falciparum - drug effects; Plasmodium falciparum - genetics; Plasmodium falciparum - physiology; Proguanil - analogs & derivatives; Proguanil - pharmacology; Proguanil - therapeutic use; Sesquiterpenes - pharmacology; Sesquiterpenes - therapeutic use
• ISSN: 1433-7851; 1521-3773
• DOI: 10.1002/anie.200200569

Approximately 40 % of the world population live in areas with the risk of malaria. Each year, 300–500 million people suffer from acute malaria, and 0.5–2.5 million die from the disease. Although malaria has been widely eradicated in many parts of the world, the global number of cases continues to rise. The most important reason for this alarming situation is the rapid spread of malaria parasites that are resistant to antimalarial drugs, especially chloroquine, which is by far the most frequently used. The development of new antimalarial drugs has been neglected since the 1970s owing to the end colonialism, changes in the areas of military engagement, and the restricted market potential. Only in recent years, in part supported by public funding programs, has interest in the development of antimalarial drugs been renewed. New data available from the recently sequenced genome of the malaria parasite Plasmodium falciparum and the application of methods of modern drug design promise to bring significant development in the fight against this disease. Increasing resistance of parasites to established therapeutics has resulted in malaria remaining one of the unsolved problems of modern medicine. Current research concentrates both on new compounds that act through established mechanisms and on new targets, such as the farnesyl transferase and the enzymes of the mevalonate‐independent isoprenoid synthesis. (See picture: erythrocyte infected with P. falciparum.)