- 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.
Bioorganic & medicinal chemistry letters (2012-12-25)
Claire-Lise Ciana, Romain Siegrist, Hamed Aissaoui, Léo Marx, Sophie Racine, Solange Meyer, Christoph Binkert, Ruben de Kanter, Christoph Fischli, Sergio Wittlin, Christoph Boss
PMID23260352
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.