Synthesis and in Vitro and in Vivo Antimalarial Activity of N-(7-Chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine Derivatives
Identifieur interne : 002040 ( Main/Exploration ); précédent : 002039; suivant : 002041Synthesis and in Vitro and in Vivo Antimalarial Activity of N-(7-Chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine Derivatives
Auteurs : Adina Ryckebusch [Belgique] ; Rébecca Deprez-Poulain [Belgique] ; Louis Maes [Belgique] ; Marie-Ange Debreu-Fontaine [Belgique] ; Elisabeth Mouray [Belgique] ; Philippe Grellier [Belgique] ; Christian Sergheraert [Belgique, France]Source :
- Journal of Medicinal Chemistry [ 0022-2623 ] ; 2003.
Abstract
Three series of monoquinolines consisting of a 1,4-bis(3-aminopropyl)piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ, and one of them cured mice infected by Plasmodium berghei.
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DOI: 10.1021/jm020960r
Affiliations:
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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="2003-01-21">2003</date><date when="2003-02-13">2003</date><biblScope unit="vol">46</biblScope><biblScope unit="issue">4</biblScope><biblScope unit="page" from="542">542</biblScope><biblScope unit="page" to="557">557</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">Three series of monoquinolines consisting of a 1,4-bis(3-aminopropyl)piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ, and one of them cured mice infected by Plasmodium berghei.</div></front></TEI><affiliations><list><country><li>Belgique</li><li>France</li></country></list><tree><country name="Belgique"><noRegion><name sortKey="Ryckebusch, Adina" sort="Ryckebusch, Adina" uniqKey="Ryckebusch A" first="Adina" last="Ryckebusch">Adina Ryckebusch</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="Deprez Poulain, Rebecca" sort="Deprez Poulain, Rebecca" uniqKey="Deprez Poulain R" first="Rébecca" last="Deprez-Poulain">Rébecca Deprez-Poulain</name><name sortKey="Grellier, Philippe" sort="Grellier, Philippe" uniqKey="Grellier P" first="Philippe" last="Grellier">Philippe Grellier</name><name sortKey="Maes, Louis" sort="Maes, Louis" uniqKey="Maes L" first="Louis" last="Maes">Louis Maes</name><name sortKey="Mouray, Elisabeth" sort="Mouray, Elisabeth" uniqKey="Mouray E" first="Elisabeth" last="Mouray">Elisabeth Mouray</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)
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