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Artemisinin—A Truly Exceptional Natural Compound and New Synthetic Bioactive Derivatives

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 March 2020) | Viewed by 6093

Special Issue Editor


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Guest Editor
Department of Chemistry, University of Cologne, Greinstr. 4, D-50939 Koeln, Germany
Interests: synthesis; medicinal chemistry; synthetic organic chemistry; medicinal and pharmaceutical chemistry; spectroscopy; natural product chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Artemisinin is “a magic drug” discovered from traditional Chinese medicine. The citation comes from the person who has truly the right to say this, Youyou Tu from the Artemisinin Research Center in Beijing and winner of the 2015 Nobel Prize in physiology or medicine (Wang et al., Engineering 2019, 5, 32–39). A synthetic chemist also agrees with “magic”, because the structure of this natural sesquiterpene peroxide is really unusual, combining a cyclic peroxide with a peracetal structure (1,2,4-trioxane) with an acetal and a lactone group that makes the molecules look highly hydrolysis-labile and redox-reactive. Following the discovery of the remarkable anti-Malaria properties of this peroxide, several derivatives with improved pharmakinetic properties were developed, especially the water-soluble artesunic acid and the reduced compounds dihydroartemisinin (DHA) and the ethers made thereof, artemether and artether. These compounds showed, in addition to their activities against malaria parasites, also antiviral and anticancer activities. Recent decades have experienced an enormous increase (>2500 papers with artemisinin in the title of publications, 2000–2018, web of science) in reports on new artemisinin-related peroxides and unexpected pharmaceutical properties for the treatment of parasitic diseases, cancer, and bacterial and viral-induced diseases.

The present Special Issue intends to collect new synthetic approaches to artemisinine derivatives, conjugates and dyads, peroxidic artemisinine model compounds with similar activity profiles or new peroxides that were synthesized in order to mimic or simply understand the mode of action of the natural product.

Prof. Axel G. Griesbeck
Guest Editor

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Keywords

  • Artemisinin
  • Medicinal chemistry
  • Artemisinin-derived compounds
  • Peroxides
  • Synthesis

Published Papers (1 paper)

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Review

18 pages, 872 KiB  
Review
Safety of Artemisinin Derivatives in the First Trimester of Pregnancy: A Controversial Story
by Sarah D’Alessandro, Elena Menegola, Silvia Parapini, Donatella Taramelli and Nicoletta Basilico
Molecules 2020, 25(15), 3505; https://doi.org/10.3390/molecules25153505 - 31 Jul 2020
Cited by 12 | Viewed by 5788
Abstract
Artemisinin combination therapy (ACT) is recommended by the World Health Organization (WHO) as first line treatment for uncomplicated malaria both in adults and children. During pregnancy, ACT is considered safe only in the second and third trimester, since animal studies have demonstrated that [...] Read more.
Artemisinin combination therapy (ACT) is recommended by the World Health Organization (WHO) as first line treatment for uncomplicated malaria both in adults and children. During pregnancy, ACT is considered safe only in the second and third trimester, since animal studies have demonstrated that artemisinin derivatives can cause foetal death and congenital malformation within a narrow time window in early embryogenesis. During this period, artemisinin derivatives induce defective embryonic erythropoiesis and vasculogenesis/angiogenesis in experimental models. However, clinical data on the safety profile of ACT in pregnant women have not shown an increased risk of miscarriage, stillbirth, or congenital malformation, nor low birth weight, associated with exposure to artemisinins in the first trimester. Although further studies are needed, the evidence collected up to now is prompting the WHO towards a change in the guidelines for the treatment of uncomplicated malaria, allowing the use of ACT also in the first trimester of pregnancy. Full article
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