4.5 Article

Artemisinin-quinoline hybrid-dimers: Synthesis and in vitro antiplasmodial activity

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 23, Pages 6975-6977

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.130

Keywords

Malaria; Dihydroartemisinin; Quinoline; Hybrid; Dimer

Funding

  1. National Research Foundation [Key International Science Capacity (KISC) Initiative]
  2. North-West University

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Novel artemisinin-quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90-110 degrees C). All compounds were obtained as the beta-isomers and were tested against both chloroquine sensitive and resistant strains of Plasmodium falciparum. Hybrid-dimer 8 showed the highest antiplasmodial activity, inheriting the optimum chain length of three carbon atoms. (C) 2010 Elsevier Ltd. All rights reserved.

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