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  • Title: Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.
    Author: Araújo NC, Barton V, Jones M, Stocks PA, Ward SA, Davies J, Bray PG, Shone AE, Cristiano ML, O'Neill PM.
    Journal: Bioorg Med Chem Lett; 2009 Apr 01; 19(7):2038-43. PubMed ID: 19251414.
    Abstract:
    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.
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