Probing the Role of the Covalent Linkage of Ferrocene into a Chloroquine Template
journal contribution
posted on 2006-07-27, 00:00 authored by Christophe Biot, Wassim Daher, Cheikh M. Ndiaye, Patricia Melnyk, Bruno Pradines, Natascha Chavain, Alain Pellet, Laurent Fraisse, Lydie Pelinski, Christian Jarry, Jacques Brocard, Jamal Khalife, Isabelle Forfar-Bares, Daniel DiveA 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 β-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.
