Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines†
Identifieur interne : 002260 ( Main/Exploration ); précédent : 002259; suivant : 002261Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines†
Auteurs : Sandrine Delarue [Belgique] ; Sophie Girault [Belgique] ; Louis Maes [Belgique] ; Marie-Ange Debreu-Fontaine [Belgique] ; Mehdi Labaeïd [Belgique] ; Philippe Grellier [Belgique] ; Christian Sergheraert [Belgique, France]Source :
- Journal of Medicinal Chemistry [ 0022-2623 ] ; 2001.
Abstract
A new series of 4-anilinoquinolines with two proton-accepting side chains has been synthesized. Antimalarial activity and levels of cytotoxicity upon both MRC-5 cells and macrophages were found to be highly dependent upon the features of these side chains. Several compounds were found to be active in the low nanomolar range, against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. From among them, a morpholino derivative cured mice infected by Plasmodium berghei and displayed a lower toxicity than amodiaquine upon mouse macrophages.
Url:
DOI: 10.1021/jm010842o
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Istex, to step Corpus: 000864
- to stream Istex, to step Curation: 000864
- to stream Istex, to step Checkpoint: 001083
- to stream Main, to step Merge: 002284
- to stream Main, to step Curation: 002260
Le document en format XML
<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title>Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines†</title><author><name sortKey="Delarue, Sandrine" sort="Delarue, Sandrine" uniqKey="Delarue S" first="Sandrine" last="Delarue">Sandrine Delarue</name></author><author><name sortKey="Girault, Sophie" sort="Girault, Sophie" uniqKey="Girault S" first="Sophie" last="Girault">Sophie Girault</name></author><author><name sortKey="Maes, Louis" sort="Maes, Louis" uniqKey="Maes L" first="Louis" last="Maes">Louis Maes</name></author><author><name sortKey="Debreu Fontaine, Marie Ange" sort="Debreu Fontaine, Marie Ange" uniqKey="Debreu Fontaine M" first="Marie-Ange" last="Debreu-Fontaine">Marie-Ange Debreu-Fontaine</name></author><author><name sortKey="Labaeid, Mehdi" sort="Labaeid, Mehdi" uniqKey="Labaeid M" first="Mehdi" last="Labaeïd">Mehdi Labaeïd</name></author><author><name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name></author><author><name sortKey="Sergheraert, Christian" sort="Sergheraert, Christian" uniqKey="Sergheraert C" first="Christian" last="Sergheraert">Christian Sergheraert</name></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:5614F3DF77932866E81DA2755E182CF706E99B45</idno><date when="2001" year="2001">2001</date><idno type="doi">10.1021/jm010842o</idno><idno type="url">https://api.istex.fr/ark:/67375/TPS-TWXK2L6P-2/fulltext.pdf</idno><idno type="wicri:Area/Istex/Corpus">000864</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">000864</idno><idno type="wicri:Area/Istex/Curation">000864</idno><idno type="wicri:Area/Istex/Checkpoint">001083</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">001083</idno><idno type="wicri:doubleKey">0022-2623:2001:Delarue S:synthesis:and:in</idno><idno type="wicri:Area/Main/Merge">002284</idno><idno type="wicri:Area/Main/Curation">002260</idno><idno type="wicri:Area/Main/Exploration">002260</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a" type="main" xml:lang="en">Synthesis and in Vitro and in Vivo Antimalarial Activity of New
4-Anilinoquinolines<ref type="bib" target="#jm010842oAF2"><hi rend="superscript">†</hi></ref></title><author><name sortKey="Delarue, Sandrine" sort="Delarue, Sandrine" uniqKey="Delarue S" first="Sandrine" last="Delarue">Sandrine Delarue</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Girault, Sophie" sort="Girault, Sophie" uniqKey="Girault S" first="Sophie" last="Girault">Sophie Girault</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Maes, Louis" sort="Maes, Louis" uniqKey="Maes L" first="Louis" last="Maes">Louis Maes</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Debreu Fontaine, Marie Ange" sort="Debreu Fontaine, Marie Ange" uniqKey="Debreu Fontaine M" first="Marie-Ange" last="Debreu-Fontaine">Marie-Ange Debreu-Fontaine</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Labaeid, Mehdi" sort="Labaeid, Mehdi" uniqKey="Labaeid M" first="Mehdi" last="Labaeïd">Mehdi Labaeïd</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation></author><author><name sortKey="Sergheraert, Christian" sort="Sergheraert, Christian" uniqKey="Sergheraert C" first="Christian" last="Sergheraert">Christian Sergheraert</name><affiliation wicri:level="1"><country xml:lang="fr">Belgique</country><wicri:regionArea>Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette,B.P. 447, 59021 Lille Cedex, France, Laboratoire de Biologie Parasitaire, IFR CNRS 63, Muséum National d'HistoireNaturelle, 61 rue Buffon, 75005 Paris, France, and Tibotec, B-32800 Mechelen</wicri:regionArea><wicri:noRegion>B-32800 Mechelen</wicri:noRegion></affiliation><affiliation></affiliation><affiliation wicri:level="1"><country wicri:rule="url">France</country></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Medicinal Chemistry</title><title level="j" type="abbrev">J. Med. Chem.</title><idno type="ISSN">0022-2623</idno><idno type="eISSN">1520-4804</idno><imprint><publisher>American Chemical Society</publisher><date type="e-published" when="2001-07-25">2001</date><date when="2001-08-16">2001</date><biblScope unit="vol">44</biblScope><biblScope unit="issue">17</biblScope><biblScope unit="page" from="2827">2827</biblScope><biblScope unit="page" to="2833">2833</biblScope></imprint><idno type="ISSN">0022-2623</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-2623</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract">A new series of 4-anilinoquinolines with two proton-accepting side chains has been synthesized. Antimalarial activity and levels of cytotoxicity upon both MRC-5 cells and macrophages were found to be highly dependent upon the features of these side chains. Several compounds were found to be active in the low nanomolar range, against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. From among them, a morpholino derivative cured mice infected by Plasmodium berghei and displayed a lower toxicity than amodiaquine upon mouse macrophages.</div></front></TEI><affiliations><list><country><li>Belgique</li><li>France</li></country></list><tree><country name="Belgique"><noRegion><name sortKey="Delarue, Sandrine" sort="Delarue, Sandrine" uniqKey="Delarue S" first="Sandrine" last="Delarue">Sandrine Delarue</name></noRegion><name sortKey="Debreu Fontaine, Marie Ange" sort="Debreu Fontaine, Marie Ange" uniqKey="Debreu Fontaine M" first="Marie-Ange" last="Debreu-Fontaine">Marie-Ange Debreu-Fontaine</name><name sortKey="Girault, Sophie" sort="Girault, Sophie" uniqKey="Girault S" first="Sophie" last="Girault">Sophie Girault</name><name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name><name sortKey="Labaeid, Mehdi" sort="Labaeid, Mehdi" uniqKey="Labaeid M" first="Mehdi" last="Labaeïd">Mehdi Labaeïd</name><name sortKey="Maes, Louis" sort="Maes, Louis" uniqKey="Maes L" first="Louis" last="Maes">Louis Maes</name><name sortKey="Sergheraert, Christian" sort="Sergheraert, Christian" uniqKey="Sergheraert C" first="Christian" last="Sergheraert">Christian Sergheraert</name></country><country name="France"><noRegion><name sortKey="Sergheraert, Christian" sort="Sergheraert, Christian" uniqKey="Sergheraert C" first="Christian" last="Sergheraert">Christian Sergheraert</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 002260 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 002260 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= ChloroquineV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= ISTEX:5614F3DF77932866E81DA2755E182CF706E99B45
|texte= Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines†
}}
| This area was generated with Dilib version V0.6.33. |  |