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Design and Synthesis of Hydroxyferroquine Derivatives with Antimalarial and Antiviral Activities

Identifieur interne : 000181 ( Hal/Checkpoint ); précédent : 000180; suivant : 000182

Design and Synthesis of Hydroxyferroquine Derivatives with Antimalarial and Antiviral Activities

Auteurs : Christophe Biot [France] ; Wassim Daher [France] ; Natascha Chavain [France] ; Thierry Fandeur [France] ; Jamal Khalife [France] ; Daniel Dive [France] ; Erik De Clercq [Belgique]

Source :

RBID : Hal:hal-00099876

Abstract

Three ferroquine (FQ) derivatives, closely mimicking the antimalarial drug hydroxychloroquine (HCQ), have been prepared. Whereas these organometallic compounds provide the expected reduced cytotoxic effects compared to FQ, they inhibit in vitro growth of Plasmodium falciparum far better than chloroquine (CQ). Moreover, this new class of bioorganometallic compounds exert antiviral effects with some selectivity toward SARS-CoV infection. These new drugs may offer an interesting alternative for Asia where SARS originated and malaria has remained endemic.


Url:
DOI: 10.1021/jm0601856

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Hal:hal-00099876

Le document en format XML

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<p>Three ferroquine (FQ) derivatives, closely mimicking the antimalarial drug hydroxychloroquine (HCQ), have been prepared. Whereas these organometallic compounds provide the expected reduced cytotoxic effects compared to FQ, they inhibit in vitro growth of Plasmodium falciparum far better than chloroquine (CQ). Moreover, this new class of bioorganometallic compounds exert antiviral effects with some selectivity toward SARS-CoV infection. These new drugs may offer an interesting alternative for Asia where SARS originated and malaria has remained endemic.</p>
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<idno type="stamp" n="RIIP">Institut Pasteur RIIP (Réseau International)</idno>
<idno type="stamp" n="UNIV-LILLE">Université de Lille</idno>
<idno type="stamp" n="INRAE">Institut National de Recherche en Agriculture, Alimentation et Environnement</idno>
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<note type="audience" n="1">Not set</note>
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<analytic>
<title xml:lang="en">Design and Synthesis of Hydroxyferroquine Derivatives with Antimalarial and Antiviral Activities</title>
<author role="aut">
<persName>
<forename type="first">Christophe</forename>
<surname>Biot</surname>
</persName>
<email type="md5">24d0649ab3920ff9444060dcdf04268d</email>
<email type="domain">ensc-lille.fr</email>
<idno type="halauthorid">129769</idno>
<affiliation ref="#struct-3209"></affiliation>
</author>
<author role="aut">
<persName>
<forename type="first">Wassim</forename>
<surname>Daher</surname>
</persName>
<idno type="halauthorid">113556</idno>
<affiliation ref="#struct-2906"></affiliation>
</author>
<author role="aut">
<persName>
<forename type="first">Natascha</forename>
<surname>Chavain</surname>
</persName>
<idno type="halauthorid">128614</idno>
<affiliation ref="#struct-3209"></affiliation>
</author>
<author role="aut">
<persName>
<forename type="first">Thierry</forename>
<surname>Fandeur</surname>
</persName>
<idno type="halauthorid">120623</idno>
<affiliation ref="#struct-20673"></affiliation>
</author>
<author role="aut">
<persName>
<forename type="first">Jamal</forename>
<surname>Khalife</surname>
</persName>
<idno type="halauthorid">113564</idno>
<affiliation ref="#struct-2906"></affiliation>
</author>
<author role="aut">
<persName>
<forename type="first">Daniel</forename>
<surname>Dive</surname>
</persName>
<idno type="halauthorid">113560</idno>
<affiliation ref="#struct-2906"></affiliation>
</author>
<author role="aut">
<persName>
<forename type="first">Erik</forename>
<surname>De Clercq</surname>
</persName>
<idno type="halauthorid">131131</idno>
<affiliation ref="#struct-20675"></affiliation>
</author>
</analytic>
<monogr>
<idno type="halJournalId" status="VALID">15785</idno>
<idno type="issn">0022-2623</idno>
<idno type="eissn">1520-4804</idno>
<title level="j">Journal of Medicinal Chemistry</title>
<imprint>
<publisher>American Chemical Society</publisher>
<biblScope unit="volume">49</biblScope>
<biblScope unit="pp">2845</biblScope>
<date type="datePub">2006</date>
</imprint>
</monogr>
<idno type="doi">10.1021/jm0601856</idno>
</biblStruct>
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<language ident="en">English</language>
</langUsage>
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<classCode scheme="halDomain" n="chim.ther">Chemical Sciences/Medicinal Chemistry</classCode>
<classCode scheme="halTypology" n="ART">Journal articles</classCode>
</textClass>
<abstract xml:lang="en">
<p>Three ferroquine (FQ) derivatives, closely mimicking the antimalarial drug hydroxychloroquine (HCQ), have been prepared. Whereas these organometallic compounds provide the expected reduced cytotoxic effects compared to FQ, they inhibit in vitro growth of Plasmodium falciparum far better than chloroquine (CQ). Moreover, this new class of bioorganometallic compounds exert antiviral effects with some selectivity toward SARS-CoV infection. These new drugs may offer an interesting alternative for Asia where SARS originated and malaria has remained endemic.</p>
</abstract>
</profileDesc>
</hal>
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