Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.

@article{Arajo2009SemisyntheticAS,
  title={Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.},
  author={Nuna C. P. Ara{\'u}jo and Victoria Barton and Michael Jones and Paul A. Stocks and Stephen A Ward and Jill Davies and Patrick G. Bray and Alison E. Shone and Maria Lurdes S Cristiano and Paul M O'neill},
  journal={Bioorganic & medicinal chemistry letters},
  year={2009},
  volume={19 7},
  pages={2038-43}
}
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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