4.7 Review

Current scenario of artemisinin and its analogues for antimalarial activity

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 163, Issue -, Pages 804-829

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.12.007

Keywords

Antimalarial drugs; Drug resistance; Malaria; Plasmodium falciparum; Plasmodium vivax

Funding

  1. Department of Science and Technology, New Delhi, India
  2. DST-SERB communication [DST-YSS/2015/001838]

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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. (C) 2018 Elsevier Masson SAS. All rights reserved.

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