Neue Leitstrukturen für Antimalariawirkstoffe? 10‐Alkylaminoartemisinin‐Derivate (siehe Beispielstruktur) zeigen in vivo eine höhere Antimalaria‐Aktivität als die Stammverbindung Artemisinin. Frühere Aussagen bezüglich der Antimalaria‐Aktivität dieser Verbindungsklasse müssen neu bewertet werden.
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.
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