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Convenient Access Both to Highly Antimalaria‐Active 10‐Arylaminoartemisinins, and to 10‐Alkyl Ethers Including Artemether, Arteether, and Artelinate
Author(s) -
Haynes Richard K.,
Chan HoWai,
Ho WingYan,
Ko Cliff KiFung,
Gerena Lucia,
Kyle Dennis E.,
Peters Wallace,
Robinson Brian L.
Publication year - 2005
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200400366
Subject(s) - artesunate , artemether , artemisinin , plasmodium berghei , alkyl , plasmodium yoelii , chemistry , in vivo , dihydroartemisinin , stereochemistry , pharmacology , combinatorial chemistry , organic chemistry , plasmodium falciparum , medicine , biology , malaria , parasitemia , microbiology and biotechnology , immunology
An economical phase‐transfer method is used to prepare 10‐arylaminoartemisinins from DHA and arylamines, and artemether, arteether, and artelinate from the corresponding alcohols. In vivo sc screens against Plasmodium berghei and P. yoelii in mice reveal that the p ‐fluorophenylamino derivative 5 g is some 13 and 70 times, respectively, more active than artesunate; this reflects the very high sc activity of 10‐alkylaminoartemisinins. However, through the po route, the compounds are less active than the alkylaminoartemisinins, but still approximately equipotent with artesunate.