Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold

  • Bioorg Med Chem Lett. 2013 Feb 1;23(3):658-62. doi: 10.1016/j.bmcl.2012.11.118.
Claire-Lise Ciana  1 ,  Romain Siegrist ,  Hamed Aissaoui ,  Léo Marx ,  Sophie Racine ,  Solange Meyer ,  Christoph Binkert ,  Ruben de Kanter ,  Christoph Fischli ,  Sergio Wittlin ,  Christoph Boss
Affiliations
  • 1. Actelion Pharmaceuticals Ltd, Drug Discovery Chemistry and Biology, Hegenheimermattweg 91, CH-4123 Allschwil/BL, Switzerland.
PMID: 23260352 DOI: 10.1016/j.bmcl.2012.11.118
Abstract

A novel series of anti-malarials, based on a hydroxy-ethyl-amine scaffold, initially identified as peptidomimetic Protease Inhibitors is described. Combination of the hydroxy-ethyl-amine anti-malarial phramacophore with the known Mannich base pharmacophore of amodiaquine (57) resulted in promising in vivo active novel derivatives.

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