Abstract

According to the World Health Organization, malaria remains one of the biggest public health problems in the world. The development of resistance is a current concern, mainly because the number of safe drugs for this disease is limited. Artemisinin-based combination therapy is recommended by the World Health Organization to prevent or delay the onset of resistance. Thus, the need to obtain new drugs makes artemisinin the most widely used scaffold to obtain synthetic compounds. This review describes the drugs based on artemisinin and its derivatives, including hybrid derivatives and dimers, trimers and tetramers that contain an endoperoxide bridge. This class of compounds is of extreme importance for the discovery of new drugs to treat malaria.

Highlights

  • Malaria is one of the most important public health problems worldwide, with almost half of the global population exposed to the risk of contamination

  • This disease is transmitted by the bite of the female mosquito of the genus Anopheles infected with the protozoa, of which five species are responsible for infecting humans: Plasmodium falciparum, P. vivax, P. malariae, P. ovale and P. knowlesi (Garcia 2010)

  • This review describes the drugs based on artemisinin and its derivatives that are recommended by the World Health Organization (WHO) for the treatment of malaria

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Summary

Introduction

Malaria is one of the most important public health problems worldwide, with almost half of the global population exposed to the risk of contamination. In the 1970s, pyronaridine (PYR 8) (Figure 2) was synthesized; a 10-phenyl aminobenzo[b][1,5] naphthyridine derivative that was active against drug-resistant P. falciparum strains (Kaur et al 2010). Since the discovery of the antimalarial activity of ART and its semi-synthetic derivatives, they have been used in the treatment of malaria as first-line drugs.

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