AI Article Synopsis
- The research presents a new, efficient method to synthesize both (-)-artemisinin and its natural counterpart (+)-artemisinin using common chemicals extracted from citronellene.
- The team investigated the action of artemisinin against the Plasmodium falciparum malaria parasite, finding that its antimalarial activity is not dependent on its molecular stereochemistry.
- This innovative approach to synthesizing artemisinin derivatives could lead to new treatments, particularly in the fight against the growing resistance of malaria parasites to existing artemisinin therapies.
Article Abstract
Here, we describe an efficient and diversity-oriented entry to both (-)-artemisinin (1) and its natural antipode (+)-artemisinin, starting from commercially and readily available S-(+)- and R-(-)-citronellene, respectively. Subsequently, we answered the still open question regarding the specificity of artemisinins action. By using a drug-sensitive Plasmodium falciparum NF54 strain, we showed that the antimalarial activity of artemisinin is not stereospecific. Our straightforward and biomimetic approach to this natural endoperoxide enables the synthesis of artemisinin derivatives that are not accessible through applying current methods and may help to address the problem of emerging resistance of Plasmodium falciparum towards artemisinin.
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| http://dx.doi.org/10.1002/anie.201802015 | DOI Listing |
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