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Probing the Role of the Covalent Linkage of Ferrocene into a Chloroquine Template

2006; American Chemical Society; Volume: 49; Issue: 15 Linguagem: Inglês

10.1021/jm060259d

1520-4804

Christophe Biot, Wassim Daher, Cheikh Ndiaye, Patricia Melnyk, Bruno Pradines, Natascha Leleu‐Chavain, Alain Pellet, Laurent Fraisse, Lydie Pélinski, Christian Jarry, Jacques Brocard, Jamal Khalife, Isabelle Forfar, Daniel Dive,

Chemical Synthesis and Analysis

A new therapeutic approach to malaria led to the discovery of ferroquine (FQ, SR97276). To assess the importance of the linkage of the ferrocenyl group to a 4-aminoquinoline scaffold, two series of 4-aminoquinolines, structurally related to FQ, were synthesized. Evaluation of antimalarial activity, physicochemical parameters, and the beta-hematin inhibition property indicate that the ferrocene moiety has to be covalently flanked by a 4-aminoquinoline and an alkylamine. Current data reinforced our choice of FQ as a drug candidate.