2. Academic Validation
  3. Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine

Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine

  • ACS Med Chem Lett. 2013 May 22;4(7):637-41. doi: 10.1021/ml400164t.
Peter M Njogu 1,  Jiri Gut 2,  Philip J Rosenthal 2,  Kelly Chibale 3
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
  • 2 Department of Medicine, San Francisco General Hospital, University of California , San Francisco, California 94143, United States.
  • 3 Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa ; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
PMID: 24900723 DOI: 10.1021/ml400164t
Abstract

A series of hybrid compounds based on (2R,3S)-N-benzoyl-3-phenylisoserine, artemisinin, and quinoline moieties was synthesized and tested for in vitro antiplasmodial activity against erythrocytic stages of K1 and W2 strains of Plasmodium falciparum. Two hybrid compounds incorporating (2R,3S)-N-benzoyl-3-phenylisoserine and artemisinin scaffolds were 3- to 4-fold more active than dihydroartemisinin, with nanomolar IC50 values against Plasmodium falciparum K1 strain.

Keywords

(2R,3S)-N-Benzoyl-3-phenylisoserine; antiplasmodial activity; artemisinin; hybrids; quinoline.

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