Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375309 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
A novel series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts.
Graphical abstractA series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields, and were evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts.Figure optionsDownload full-size imageDownload as PowerPoint slide