Synthesis and antimalarial activities of several fluorinated artemisinin derivatives.
The carbonyl groups in several artemisinin derivatives were converted into geminal difluorinated compounds on treatment with diethylaminosulfur trifluoride. A number of other mono- and polyfluorinated artemisinin derivatives were prepared. Their in vitro antimalarial activities were all equal to or greater than the nonfluorinated analogs or precursors.
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Laboratory of Chemical Physics, NIDDK, Bethesda, Maryland 20892-0510, USA.
Torok
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Ziffer
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Pan
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Meshnick
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D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D037621:Artemisinins; D005461:Fluorine; D010963:Plasmodium falciparum / Q000187:drug effects; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; D005461:Fluorine; C031327:artemisinin