Probing the Role of the Covalent Linkage of Ferrocene into a Chloroquine Template
Journal of Medicinal Chemistry2006Vol. 49(15), pp. 4707–4714
Citations Over TimeTop 10% of 2006 papers
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
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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