ChloroquineV1, France, Analysis, bibRecord, 000083

Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives

Identifieur interne : 000083 ( France/Analysis ); précédent : 000082; suivant : 000084

Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives

Auteurs : Aliasghar Jarrahpour ; Malihe Aye ; Javad Ameri Rad ; Saeed Yousefinejad [Iran] ; Veronique Sinou [France] ; Christine Latour [France] ; Jean Michel Brunel [France] ; Edward Turos

Source :

Journal- Iranian Chemical Society [ 1735-207X ] ; 2018.

RBID : Hal:hal-02143574

Abstract

This paper describes the synthesis of some new beta-lactam derivatives containing the 1,2,3-triazole moiety. All the compounds were evaluated for their in vitro antimicrobial and antimalarial activities. Moderate to excellent antimalarial activities were encountered. The results showed that compounds 5a, 5c, 5f, 5i exhibited the most potent antimalarial activity with IC50 values of 0.85, < 0.97, < 0.97, 1.81 mu M against chloroquine-resistant P. falciparum K1 strain. A QSAR study highlights the structure-activity relationships that correlate the observed antimalarial activities with changes in the compounds' structural features.

Url:

https://hal-amu.archives-ouvertes.fr/hal-02143574

DOI: 10.1007/s13738-018-1330-2

Affiliations:

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

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Links to Exploration step

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Le document en format XML

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            </address>
          </desc>
          <listRelation>            <relation name="UMR_S1261" active="#struct-198056" type="direct"></relation>
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        <tutelles><tutelle name="UMR_S1261" active="#struct-198056" type="direct"><org type="institution" xml:id="struct-198056" status="VALID">          <idno type="IdRef">15863621X</idno>
          <idno type="ISNI">0000 0001 2176 4817</idno>
          <orgName>Aix Marseille Université</orgName>
          <orgName type="acronym">AMU</orgName>
          <date type="start">2012-01-01</date>
          <desc>            <address>              <addrLine>Aix-Marseille UniversitéJardins du Pharo58 Boulevard Charles Livon13284 Marseille cedex 7</addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">http://www.univ-amu.fr/</ref>
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</tutelle>
<tutelle name="UMR_S1261" active="#struct-303623" type="direct"><org type="institution" xml:id="struct-303623" status="VALID">          <idno type="IdRef">026388278</idno>
          <orgName>Institut National de la Santé et de la Recherche Médicale</orgName>
          <orgName type="acronym">INSERM</orgName>
          <desc>            <address>              <addrLine>101, rue de Tolbiac, 75013 Paris </addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">http://www.inserm.fr</ref>
          </desc>
        </org>
</tutelle>
<tutelle name="UMR_S1261" active="#struct-507058" type="direct"><org type="institution" xml:id="struct-507058" status="VALID">          <orgName>Institut de Recherche Biomédicale des Armées</orgName>
          <orgName type="acronym">IRBA</orgName>
          <desc>            <address>              <addrLine>Brétigny-sur-Orge</addrLine>
              <country key="FR"></country>
            </address>
            <ref type="url">https://www.defense.gouv.fr/sante/notre-expertise/recherche-biomedicale/recherche-biomedicale</ref>
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</tutelle>
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</hal:affiliation>
<country>France</country>
<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>
</affiliation>
</author>
<author><name sortKey="Turos, Edward" sort="Turos, Edward" uniqKey="Turos E" first="Edward" last="Turos">Edward Turos</name>
</author>
</analytic>
<idno type="DOI">10.1007/s13738-018-1330-2</idno>
<series><title level="j">Journal- Iranian Chemical Society</title>
<idno type="ISSN">1735-207X</idno>
<imprint><date type="datePub">2018</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
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<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">              <p>This paper describes the synthesis of some new beta-lactam derivatives containing the 1,2,3-triazole moiety. All the compounds were evaluated for their in vitro antimicrobial and antimalarial activities. Moderate to excellent antimalarial activities were encountered. The results showed that compounds 5a, 5c, 5f, 5i exhibited the most potent antimalarial activity with IC50 values of 0.85, < 0.97, < 0.97, 1.81 mu M against chloroquine-resistant P. falciparum K1 strain. A QSAR study highlights the structure-activity relationships that correlate the observed antimalarial activities with changes in the compounds' structural features.</p>
            </div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
<li>Iran</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><noCountry><name sortKey="Aye, Malihe" sort="Aye, Malihe" uniqKey="Aye M" first="Malihe" last="Aye">Malihe Aye</name>
<name sortKey="Jarrahpour, Aliasghar" sort="Jarrahpour, Aliasghar" uniqKey="Jarrahpour A" first="Aliasghar" last="Jarrahpour">Aliasghar Jarrahpour</name>
<name sortKey="Rad, Javad Ameri" sort="Rad, Javad Ameri" uniqKey="Rad J" first="Javad Ameri" last="Rad">Javad Ameri Rad</name>
<name sortKey="Turos, Edward" sort="Turos, Edward" uniqKey="Turos E" first="Edward" last="Turos">Edward Turos</name>
</noCountry>
<country name="Iran"><noRegion><name sortKey="Yousefinejad, Saeed" sort="Yousefinejad, Saeed" uniqKey="Yousefinejad S" first="Saeed" last="Yousefinejad">Saeed Yousefinejad</name>
</noRegion>
</country>
<country name="France"><region name="Provence-Alpes-Côte d'Azur"><name sortKey="Sinou, Veronique" sort="Sinou, Veronique" uniqKey="Sinou V" first="Veronique" last="Sinou">Veronique Sinou</name>
</region>
<name sortKey="Brunel, Jean Michel" sort="Brunel, Jean Michel" uniqKey="Brunel J" first="Jean Michel" last="Brunel">Jean Michel Brunel</name>
<name sortKey="Latour, Christine" sort="Latour, Christine" uniqKey="Latour C" first="Christine" last="Latour">Christine Latour</name>
</country>
</tree>
</affiliations>
</record>

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Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives

Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives

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