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. 2006 Jul 27;49(15):4707-14.
doi: 10.1021/jm060259d.

Probing the role of the covalent linkage of ferrocene into a chloroquine template

Christophe Biot  1 , 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 Dive
Affiliations

Probing the role of the covalent linkage of ferrocene into a chloroquine template

Christophe Biot et al. J Med Chem. .

Abstract

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.

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