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

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 i...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-02, Vol.23 (3), p.658-662
Main Authors: Ciana, Claire-Lise, Siegrist, Romain, Aissaoui, Hamed, Marx, Léo, Racine, Sophie, Meyer, Solange, Binkert, Christoph, de Kanter, Ruben, Fischli, Christoph, Wittlin, Sergio, Boss, Christoph
Format: Article
Language:English
Subjects:
Animals
antimalarials
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Aspartic Acid Endopeptidases - metabolism
chemistry
Disease Models, Animal
Dual mechanism of action
Ethylamines - chemistry
Ethylamines - pharmacology
Hydroxylamine - chemistry
Hydroxylamine - pharmacology
Inhibitory Concentration 50
Malaria
Malaria - drug therapy
Mannich base
Medicinal chemistry
Mice
Molecular Structure
pharmacology
Plasmodium berghei - drug effects
proteinase inhibitors
Speed of action
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.11.118