title: Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold.
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.
authors.affiliation: Actelion Pharmaceuticals Ltd, Drug Discovery Chemistry and Biology, Hegenheimermattweg 91, CH-4123 Allschwil/BL, Switzerland.
authors.forename: Claire-Lise
authors.initials: CL
authors.lastname: Ciana
authors.forename: Romain
authors.initials: R
authors.lastname: Siegrist
authors.forename: Hamed
authors.initials: H
authors.lastname: Aissaoui
authors.forename: Léo
authors.initials: L
authors.lastname: Marx
authors.forename: Sophie
authors.initials: S
authors.lastname: Racine
authors.forename: Solange
authors.initials: S
authors.lastname: Meyer
authors.forename: Christoph
authors.initials: C
authors.lastname: Binkert
authors.forename: Ruben
authors.initials: R
authors.lastname: de Kanter
authors.forename: Christoph
authors.initials: C
authors.lastname: Fischli
authors.forename: Sergio
authors.initials: S
authors.lastname: Wittlin
authors.forename: Christoph
authors.initials: C
authors.lastname: Boss
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000378:metabolism; D004195:Disease Models, Animal; D005021:Ethylamines / Q000737:chemistry* / Q000494:pharmacology; D019811:Hydroxylamine / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D015394:Molecular Structure; D010962:Plasmodium berghei / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D005021:Ethylamines; D019811:Hydroxylamine; D016282:Aspartic Acid Endopeptidases; C089643:plasmepsin