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Fluoroartemisinins: Metabolically More Stable Antimalarial Artemisinin Derivatives
Author(s) -
Bégué JeanPierre,
BonnetDelpon Danièle
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600156
Subject(s) - artemisinin , trifluoromethyl , fluorine , chemistry , combinatorial chemistry , substitution (logic) , pharmacology , plasmodium falciparum , malaria , organic chemistry , medicine , computer science , alkyl , immunology , programming language
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.