Serveur d'exploration Chloroquine

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

Identifieur interne : 000328 ( France/Analysis ); précédent : 000327; suivant : 000329

Probing 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 :

RBID : Hal:hal-00097346

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:


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Hal:hal-00097346

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<idno type="DOI">10.1021/jm060259d</idno>
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<title level="j">Journal of Medicinal Chemistry</title>
<idno type="ISSN">0022-2623</idno>
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<date type="datePub">2006</date>
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<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>
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<name sortKey="Fraisse, Laurent" sort="Fraisse, Laurent" uniqKey="Fraisse L" first="Laurent" last="Fraisse">Laurent Fraisse</name>
<name sortKey="Jarry, Christian" sort="Jarry, Christian" uniqKey="Jarry C" first="Christian" last="Jarry">Christian Jarry</name>
<name sortKey="Khalife, Jamal" sort="Khalife, Jamal" uniqKey="Khalife J" first="Jamal" last="Khalife">Jamal Khalife</name>
<name sortKey="M Ndiaye, Cheikh" sort="M Ndiaye, Cheikh" uniqKey="M Ndiaye C" first="Cheikh" last="M. Ndiaye">Cheikh M. Ndiaye</name>
<name sortKey="Melnyk, Patricia" sort="Melnyk, Patricia" uniqKey="Melnyk P" first="Patricia" last="Melnyk">Patricia Melnyk</name>
<name sortKey="Pelinski, Lydie" sort="Pelinski, Lydie" uniqKey="Pelinski L" first="Lydie" last="Pelinski">Lydie Pelinski</name>
<name sortKey="Pellet, Alain" sort="Pellet, Alain" uniqKey="Pellet A" first="Alain" last="Pellet">Alain Pellet</name>
<name sortKey="Pradines, Bruno" sort="Pradines, Bruno" uniqKey="Pradines B" first="Bruno" last="Pradines">Bruno Pradines</name>
</country>
</tree>
</affiliations>
</record>

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   |texte=   Probing the role of the covalent linkage of ferrocene into a chloroquine template
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