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Discovery of dual function acridones as a new antimalarial chemotype

Author

Listed:
  • Jane X. Kelly

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Portland State University, Portland, Oregon 97201, USA)

  • Martin J. Smilkstein

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Portland State University, Portland, Oregon 97201, USA
    Oregon Health and Science University, Portland, Oregon 97239, USA
    Present addresses: Oregon Translational Research and Drug Development Institute, Portland, Oregon 97201, USA (M.J.S.); Department of Microbiology and Immunology, Virginia Commonwealth University, Richmond, Virginia 23298, USA (K.D.L.).)

  • Reto Brun

    (Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland)

  • Sergio Wittlin

    (Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland)

  • Roland A. Cooper

    (Old Dominion University, Norfolk, Virginia 23529, USA)

  • Kristin D. Lane

    (Old Dominion University, Norfolk, Virginia 23529, USA
    Present addresses: Oregon Translational Research and Drug Development Institute, Portland, Oregon 97201, USA (M.J.S.); Department of Microbiology and Immunology, Virginia Commonwealth University, Richmond, Virginia 23298, USA (K.D.L.).)

  • Aaron Janowsky

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Oregon Health and Science University, Portland, Oregon 97239, USA)

  • Robert A. Johnson

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Oregon Health and Science University, Portland, Oregon 97239, USA)

  • Rozalia A. Dodean

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Portland State University, Portland, Oregon 97201, USA)

  • Rolf Winter

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Portland State University, Portland, Oregon 97201, USA)

  • David J. Hinrichs

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Oregon Health and Science University, Portland, Oregon 97239, USA)

  • Michael K. Riscoe

    (Portland Veterans Affairs Medical Centre, Portland, Oregon 97239, USA
    Portland State University, Portland, Oregon 97201, USA
    Oregon Health and Science University, Portland, Oregon 97239, USA)

Abstract

New ways with antimalarials The emergence of drug resistance is a continued problem in the battle against malaria. A new class of antimalarial could help to counteract that problem by making possible a novel approach to combination therapy. The dual function acridone compounds combine the haem-targeting antimalarial action of conventional antimalarial acridones with a second active region in the molecule. This boosts the efficacy of established antimalarials such as chloroquine, amodiaquine, quinine and piperaquine synergistically, in some instances overcoming prior resistance to some of these drugs in the Plasmodium falciparum parasites.

Suggested Citation

  • Jane X. Kelly & Martin J. Smilkstein & Reto Brun & Sergio Wittlin & Roland A. Cooper & Kristin D. Lane & Aaron Janowsky & Robert A. Johnson & Rozalia A. Dodean & Rolf Winter & David J. Hinrichs & Mich, 2009. "Discovery of dual function acridones as a new antimalarial chemotype," Nature, Nature, vol. 459(7244), pages 270-273, May.
    • Handle: RePEc:nat:nature:v:459:y:2009:i:7244:d:10.1038_nature07937
    DOI: 10.1038/nature07937
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