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ARTEMISININ DERIVATIVES IN THE TREATMENT OF MALARIA |
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Principal Investigator: J-P. BEGUE
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TECHNICAL DESCRIPTION
This invention describes the fluorinated analogs of Artemisinin designed by introducing a fluoroalkyl group to protect Artemisinin derivatives against the metabolism. These fluroalkyl DHA derivatives are more active than artemether and artesunate in-vivo in mice : 100 % survival and no recurrence of parasitemia. The technology also involves a method to design and synthesize new F-ART derivatives substituted by a fluorinated substitute at C-10 and by another function at C-16 to improve water solubility, and to perform in vitro and in vivo tests on these artemisin derivatives.
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