Current scenario of artemisinin and its analogues for antimalarial activity

Eur J Med Chem. 2019 Feb 1:163:804-829. doi: 10.1016/j.ejmech.2018.12.007. Epub 2018 Dec 13.

Abstract

Human malaria, one of the most striking, reemerging infectious diseases, is caused by several types of Plasmodium parasites. Whilst advances have been made in lowering the numbers of cases and deaths, it is clear that a strategy based solely on disease control year on year, without reducing transmission and ultimately eradicating the parasite, is unsustainable. Natural products have served as a template for the design and development of antimalarial drugs currently in the clinic or in the development phase. Artemisinin combine potent, rapid antimalarial activity with a wide therapeutic index and an absence of clinically important resistance. The alkylating ability of artemisinin and its semi-synthetic analogues toward heme related to their antimalarial efficacy are underlined. Although impressive results have already been achieved in malaria research, more systematization and concentration of efforts are required if real breakthroughs are to be made. This review will concisely cover the clinical, preclinical antimalarial and current updates in artemisinin based antimalarial drugs. Diverse classes of semi-synthetic analogs of artemisinin reported in the last decade have also been extensively studied. The experience gained in this respect is discussed.

Keywords: Antimalarial drugs; Drug resistance; Malaria; Plasmodium falciparum; Plasmodium vivax.

Publication types

  • Review

MeSH terms

  • Antimalarials / pharmacology*
  • Artemisinins / chemistry
  • Artemisinins / therapeutic use*
  • Humans
  • Malaria / drug therapy*
  • Plasmodium / drug effects

Substances

  • Antimalarials
  • Artemisinins
  • artemisinin