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History of Antimalarial Agents

  1. David Greenwood

Published Online: 15 SEP 2009

DOI: 10.1002/9780470015902.a0003624.pub2



How to Cite

Greenwood, D. 2009. History of Antimalarial Agents. eLS. .

Author Information

  1. University of Nottingham, Nottingham, UK

Publication History

  1. Published Online: 15 SEP 2009

This is not the most recent version of the article. View current version (14 APR 2015)


Malaria is a debilitating and, in its most severe form, falciparum malaria, a potentially fatal disease. Treatment in the form of powdered bark of the cinchona tree from South America has been available from at least the seventeenth century. Synthetic antimalarial agents were not developed until the twentieth century, stimulated by serious shortages of supply during the two World Wars. The first advances were made in Germany in the interwar period. During and after World War II, further progress was made in Britain and the United States. Inevitably resistance to these agents emerged and became a major problem after the 1960s. Other active chemicals have since been developed, but many have serious side effects and much hope is now pinned on derivatives of a natural product, artemisinin, obtained from sweet wormwood (Artemisia annua) and used for centuries (though not at first for malaria) in traditional Chinese medicine.

Key Concepts

  • Malaria is a potentially fatal disease affecting millions of people, chiefly in tropical countries.

  • A treatment in the form of powdered bark of the cinchona tree from northern South America has been available since the seventeenth century.

  • Cinchona bark contains several antimalarial alkaloids, most importantly quinine.

  • Synthetic antimalarial agents were first developed in Germany in the 1920s and 1930s.

  • The first antifolate compound active against malaria, proguanil, was developed in England during World War II.

  • After World War II, several important synthetic antimalarial compounds, notably chloroquine and pyrimethamine became available for prophylaxis and treatment.

  • From the 1960s resistance emerged as a major issue and quinine once again became the treatment of choice for serious falciparum malaria.

  • Derivatives of artemisinin, a natural product used in traditional Chinese medicine, is being now being successfully used in treatment.


  • antimalarial agents;
  • quinine;
  • cinchona bark;
  • chloroquine;
  • artemisinin