| Literature DB >> 16854077 |
Christophe Biot1, 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.
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.Entities:
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Year: 2006 PMID： 16854077 DOI： 10.1021/jm060259d
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446