ChloroquineV1, France, Analysis, bibRecord, 000068

Design and synthesis of simplified speciophylline analogues and β-carbolines as active molecules against Plasmodium falciparum

Identifieur interne : 000068 ( France/Analysis ); précédent : 000067; suivant : 000069

Design and synthesis of simplified speciophylline analogues and β-carbolines as active molecules against Plasmodium falciparum

Auteurs : David Pierrot [France] ; Véronique Sinou [France] ; Sok-Siya Bun [France] ; Daniel Parzy [France] ; Nicolas Taudon [France] ; Jean Rodriguez [France] ; Evelyne Ollivier [France] ; Damien Bonne [France]

Source :

RBID : Hal:medihal-02087312

English descriptors

mix :
- antimalarial activity, speciophylline, spirooxindoles, β-carbolines.

Abstract

A structure–activity relationship study of active molecules against chloroquine‐resistant Plasmodium falciparum K1 strain is reported. Structurally simplified analogues of antiplasmodial active alkaloids presented similar levels of activity as their corresponding natural products extracted from Guiera senegalensis and Mitragyna inermis with IC50 values on chloroquine‐resistant P. falciparum K1 strain of up to 10.6 μM for spirooxindoles and 13.8 μM for β‐carbolines. The identification of such simpler and cheaper structural analogues is crucial to efficiently study these natural products' action mode as well as developing new cures against malaria.

Url:

https://medihal.archives-ouvertes.fr/medihal-02087312

Affiliations:

Links toward previous steps (curation, corpus...)

to stream Hal, to step Corpus: 000065
to stream Hal, to step Curation: 000065
to stream Hal, to step Checkpoint: 000018
to stream Main, to step Merge: 000B81
to stream Main, to step Curation: 000B81
to stream Main, to step Exploration: 000B81
to stream France, to step Extraction: 000068

Links to Exploration step

Hal:medihal-02087312

Le document en format XML

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<author><name sortKey="Ollivier, Evelyne" sort="Ollivier, Evelyne" uniqKey="Ollivier E" first="Evelyne" last="Ollivier">Evelyne Ollivier</name>
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<author><name sortKey="Bonne, Damien" sort="Bonne, Damien" uniqKey="Bonne D" first="Damien" last="Bonne">Damien Bonne</name>
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<placeName><settlement type="city">Marseille</settlement>
<region type="region" nuts="2">Provence-Alpes-Côte d'Azur</region>
</placeName>
<orgName type="university">Université d'Aix-Marseille</orgName>
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</analytic>
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</sourceDesc>
</fileDesc>
<profileDesc><textClass><keywords scheme="mix" xml:lang="en"><term>antimalarial activity</term>
<term>speciophylline</term>
<term>spirooxindoles</term>
<term>β-carbolines</term>
</keywords>
</textClass>
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</teiHeader>
<front><div type="abstract" xml:lang="en">              <p>A structure–activity relationship study of active molecules against chloroquine‐resistant Plasmodium falciparum K1 strain is reported. Structurally simplified analogues of antiplasmodial active alkaloids presented similar levels of activity as their corresponding natural products extracted from Guiera senegalensis and Mitragyna inermis with IC50 values on chloroquine‐resistant P. falciparum K1 strain of up to 10.6 μM for spirooxindoles and 13.8 μM for β‐carbolines. The identification of such simpler and cheaper structural analogues is crucial to efficiently study these natural products' action mode as well as developing new cures against malaria.</p>
            </div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
</country>
<region><li>Provence-Alpes-Côte d'Azur</li>
</region>
<settlement><li>Marseille</li>
</settlement>
<orgName><li>Université d'Aix-Marseille</li>
</orgName>
</list>
<tree><country name="France"><region name="Provence-Alpes-Côte d'Azur"><name sortKey="Pierrot, David" sort="Pierrot, David" uniqKey="Pierrot D" first="David" last="Pierrot">David Pierrot</name>
</region>
<name sortKey="Bonne, Damien" sort="Bonne, Damien" uniqKey="Bonne D" first="Damien" last="Bonne">Damien Bonne</name>
<name sortKey="Bun, Sok Siya" sort="Bun, Sok Siya" uniqKey="Bun S" first="Sok-Siya" last="Bun">Sok-Siya Bun</name>
<name sortKey="Ollivier, Evelyne" sort="Ollivier, Evelyne" uniqKey="Ollivier E" first="Evelyne" last="Ollivier">Evelyne Ollivier</name>
<name sortKey="Parzy, Daniel" sort="Parzy, Daniel" uniqKey="Parzy D" first="Daniel" last="Parzy">Daniel Parzy</name>
<name sortKey="Rodriguez, Jean" sort="Rodriguez, Jean" uniqKey="Rodriguez J" first="Jean" last="Rodriguez">Jean Rodriguez</name>
<name sortKey="Sinou, Veronique" sort="Sinou, Veronique" uniqKey="Sinou V" first="Véronique" last="Sinou">Véronique Sinou</name>
<name sortKey="Taudon, Nicolas" sort="Taudon, Nicolas" uniqKey="Taudon N" first="Nicolas" last="Taudon">Nicolas Taudon</name>
</country>
</tree>
</affiliations>
</record>

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   |wiki=    Sante
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   |texte=   Design and synthesis of simplified speciophylline analogues and β-carbolines as active molecules against Plasmodium falciparum
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Design and synthesis of simplified speciophylline analogues and β-carbolines as active molecules against Plasmodium falciparum

Design and synthesis of simplified speciophylline analogues and β-carbolines as active molecules against Plasmodium falciparum

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