Synthesis and antimalarial activity of new amino analogues of amodiaquine.
Identifieur interne : 000293 ( France/Analysis ); précédent : 000292; suivant : 000294Synthesis and antimalarial activity of new amino analogues of amodiaquine.
Auteurs : E. Paunescu [France] ; Sophie Susplugas [France] ; E. Boll ; R. Varga ; Elisabeth Mouray [France] ; Philippe Grellier [France] ; Patricia Melnyk [France]Source :
- Medicinal Chemistry [ 1573-4064 ] ; 2008.
Abstract
Amodiaquine remains one of the most prescribed antimalarial 4-aminoquinoline. To assess the importance of the 4'-hydroxyl group and subsequent hydrogen bond in the antimalarial activity of amodiaquine (AQ), a series of new analogues in which this functionality was replaced by various amino groups was synthesized. The incorporation of a 3'-pyrrolidinamino group instead of the 3'-diethylamino function of AQ allowed the development of a parallel series of amopyroquine derivatives. The compounds were screened against both chloroquine (CQ)-sensitive and -resistant strains of Plasmodium falciparum and their cytotoxicity evaluated upon the MRC5 cell line. Antimalarial activity in a low nanomolar range was recorded showing that the 4'-hydroxy function can be successfully replaced by various amino substituents in terms of activity without any influence of the level of CQ-resistance of the strains. Furthermore the ability of the compounds to inhibit beta-hematin formation was measured in order to discuss the mechanism of action of these new compounds. Compounds 7d and 8d exhibit a high selectivity index and may be considered as promising leads for further development.
Url:
DOI: 10.2174/157340608785700153
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Hal, to step Corpus: 000223
- to stream Hal, to step Curation: 000223
- to stream Hal, to step Checkpoint: 000216
- to stream Main, to step Merge: 001933
- to stream Main, to step Curation: 001927
- to stream Main, to step Exploration: 001927
- to stream France, to step Extraction: 000293
Links to Exploration step
Hal:mnhn-02070086Le document en format XML
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<desc> <address> <addrLine>57 rue Cuvier - 75005 Paris</addrLine>
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<orgName type="acronym">MNHN</orgName>
<desc> <address> <addrLine>57, rue Cuvier - 75231 Paris Cedex 05</addrLine>
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<ref type="url">http://www.mnhn.fr</ref>
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<orgName>Centre National de la Recherche Scientifique</orgName>
<orgName type="acronym">CNRS</orgName>
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<country>France</country>
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<author><name sortKey="Melnyk, Patricia" sort="Melnyk, Patricia" uniqKey="Melnyk P" first="Patricia" last="Melnyk">Patricia Melnyk</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-24511" status="OLD"> <orgName>Institut de biologie de Lille - IBL</orgName>
<orgName type="acronym">IBLI</orgName>
<desc> <address> <addrLine>Institut de Biologie de Lille 1 Rue du Professeur Calmette - 447 59021 LILLE CEDEX</addrLine>
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<orgName>Université de Lille, Sciences et Technologies</orgName>
<date type="end">2017-12-31</date>
<desc> <address> <addrLine>Cité Scientifique - 59655 Villeneuve d'Ascq Cedex</addrLine>
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<tutelle active="#struct-300166" type="direct"><org type="institution" xml:id="struct-300166" status="VALID"> <orgName>Institut Pasteur de Lille</orgName>
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<ref type="url">https://research.pasteur.fr/ip-network</ref>
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<orgName>Université de Lille, Droit et Santé</orgName>
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<desc> <address> <addrLine>42 rue Paul Duez 59000 Lille</addrLine>
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<country>France</country>
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</analytic>
<idno type="DOI">10.2174/157340608785700153</idno>
<series><title level="j">Medicinal Chemistry</title>
<idno type="ISSN">1573-4064</idno>
<imprint><date type="datePub">2008</date>
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<front><div type="abstract" xml:lang="en"> <p>Amodiaquine remains one of the most prescribed antimalarial 4-aminoquinoline. To assess the importance of the 4'-hydroxyl group and subsequent hydrogen bond in the antimalarial activity of amodiaquine (AQ), a series of new analogues in which this functionality was replaced by various amino groups was synthesized. The incorporation of a 3'-pyrrolidinamino group instead of the 3'-diethylamino function of AQ allowed the development of a parallel series of amopyroquine derivatives. The compounds were screened against both chloroquine (CQ)-sensitive and -resistant strains of Plasmodium falciparum and their cytotoxicity evaluated upon the MRC5 cell line. Antimalarial activity in a low nanomolar range was recorded showing that the 4'-hydroxy function can be successfully replaced by various amino substituents in terms of activity without any influence of the level of CQ-resistance of the strains. Furthermore the ability of the compounds to inhibit beta-hematin formation was measured in order to discuss the mechanism of action of these new compounds. Compounds 7d and 8d exhibit a high selectivity index and may be considered as promising leads for further development.</p>
</div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
</country>
</list>
<tree><noCountry><name sortKey="Boll, E" sort="Boll, E" uniqKey="Boll E" first="E" last="Boll">E. Boll</name>
<name sortKey="Varga, R" sort="Varga, R" uniqKey="Varga R" first="R" last="Varga">R. Varga</name>
</noCountry>
<country name="France"><noRegion><name sortKey="Paunescu, E" sort="Paunescu, E" uniqKey="Paunescu E" first="E" last="Paunescu">E. Paunescu</name>
</noRegion>
<name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name>
<name sortKey="Melnyk, Patricia" sort="Melnyk, Patricia" uniqKey="Melnyk P" first="Patricia" last="Melnyk">Patricia Melnyk</name>
<name sortKey="Mouray, Elisabeth" sort="Mouray, Elisabeth" uniqKey="Mouray E" first="Elisabeth" last="Mouray">Elisabeth Mouray</name>
<name sortKey="Susplugas, Sophie" sort="Susplugas, Sophie" uniqKey="Susplugas S" first="Sophie" last="Susplugas">Sophie Susplugas</name>
</country>
</tree>
</affiliations>
</record>
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