Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.

@article{Kelly2007DesignSA,
  title={Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.},
  author={Jane Xu Kelly and Martin J. Smilkstein and Roland Arthur Cooper and Kristin Downie Lane and Robert A. Johnson and Aaron J Janowsky and Rozalia A. Dodean and David John Hinrichs and Robert W. Winter and Michael Kevin Riscoe},
  journal={Antimicrobial agents and chemotherapy},
  year={2007},
  volume={51 11},
  pages={
          4133-40
        }
}
A series of novel 10-N-substituted acridones, bearing alkyl side chains with tertiary amine groups at the terminal position, were designed, synthesized, and evaluated for the ability to enhance the potency of quinoline drugs against multidrug-resistant (MDR) Plasmodium falciparum malaria parasites. A number of acridone derivatives, with side chains bridged three or more carbon atoms apart between the ring nitrogen and terminal nitrogen, demonstrated chloroquine (CQ)-chemosensitizing activity… CONTINUE READING

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