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J Med Chem. 2006 Jul 27;49(15):4707-14.

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

Author information

1
Unité de Catalyse et Chimie du Solide - UMR CNRS 8181, ENSCL, Bâtiment C7, USTL, B.P. 90108, 59652, Villeneuve d' Ascq Cedex, France. christophe.biot@ensc-lille.fr

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.

PMID:
16854077
DOI:
10.1021/jm060259d
[Indexed for MEDLINE]

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