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Article Dans Une Revue Journal of Medicinal Chemistry Année : 2006

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

Résumé

A new therapeutic approach to malaria led to the discovery of ferroquine (FQ). 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 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.

Dates et versions

hal-00097346 , version 1 (21-09-2006)

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Christophe Biot, Wassim Daher, Cheikh M. Ndiaye, Patricia Melnyk, Bruno Pradines, et al.. Probing the role of the covalent linkage of ferrocene into a chloroquine template. Journal of Medicinal Chemistry, 2006, 49, pp.4707-4714. ⟨10.1021/jm060259d⟩. ⟨hal-00097346⟩
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