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Published on: October 11, 2019
Fluoroartemisinins: metabolically more stable antimalarial artemisinin derivatives
Jean-Pierre Bégué1, Danièle Bonnet-Delpon
1BIOCIS-UMR-CNRS-8086, Faculté de Pharmacie, 2 Rue J.B. Clément, Chatenay-Malabry, 92296, France.
Abstract:
This report is an overview on the design, preparation, and evaluation of metabolically stable artemisinins, using fluorine substitution. The chemical challenges encountered for the incorporation of fluorine-containing elements and the preparation of a large range of 10-trifluoromethyl artemisinin derivatives are detailed. Impact of the fluorine substitution on the antimalarial activity is also highlighted. Preclinical data of lead compounds, and evidence for their strong and prolonged antimalarial activity are presented.
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