Probing the role of the covalent linkage of ferrocene into a chloroquine template
Identifieur interne : 000328 ( France/Analysis ); précédent : 000327; suivant : 000329Probing the role of the covalent linkage of ferrocene into a chloroquine template
Auteurs : Christophe Biot [France] ; Wassim Daher [France] ; Cheikh M. Ndiaye [France] ; Patricia Melnyk [France] ; Bruno Pradines [France] ; Natascha Chavain [France] ; Alain Pellet [France] ; Laurent Fraisse [France] ; Lydie Pelinski [France] ; Christian Jarry [France] ; Jacques Brocard [France] ; Jamal Khalife [France] ; Isabelle Forfar-Bares [France] ; Daniel Dive [France]Source :
- Journal of Medicinal Chemistry [ 0022-2623 ] ; 2006.
Abstract
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.
Url:
DOI: 10.1021/jm060259d
Affiliations:
Links toward previous steps (curation, corpus...)
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Hal:hal-00097346Le document en format XML
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<idno type="DOI">10.1021/jm060259d</idno>
<series><title level="j">Journal of Medicinal Chemistry</title>
<idno type="ISSN">0022-2623</idno>
<imprint><date type="datePub">2006</date>
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<front><div type="abstract" xml:lang="en"> <p>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.</p>
</div>
</front>
</TEI>
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