2. Academic Validation
  3. Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold

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

Affiliation

  • 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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