ChloroquineV1, PascalFrancis, Corpus, bibRecord, 000028

Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline

Identifieur interne : 000028 ( PascalFrancis/Corpus ); précédent : 000027; suivant : 000029

Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline

Auteurs : Sandrine Delarue-Cochin ; Philippe Grellier ; Louis Maes ; Elisabeth Mouray ; Christian Sergheraert ; Patricia Melnyk

Source :

European journal of medicinal chemistry [ 0223-5234 ] ; 2008.

RBID : Pascal:08-0535287

Descripteurs français

Pascal (Inist)
- Synthèse chimique, Antipaludique, Relation structure activité, Carbamate organique, Carboxamide, Dérivé de l'aniline, Dérivé de la quinoléine, Plasmodium falciparum, Amodiaquine, Hétérocycle azote, Dérivé du benzène, Composé bicyclique, Cycle 6 chaînons, In vitro, In vivo, Chimiothérapie, Plasmodium berghei, Toxicité, Cytotoxicité, Composé aromatique, Voie orale, Paludisme, Souris, Antiparasitaire, Antiprotozoaire, Amine aromatique, Foetus, Poumon, Homme, Lignée cellulaire, Animal, Pipéridine-1-acétamide dérivé, Lignée MRC5.

English descriptors

KwdEn :
- Amodiaquine, Aniline derivatives, Animal, Antimalarial, Antiprotozoal agent, Aromatic amine, Aromatic compound, Benzene derivatives, Bicyclic compound, Carboxamide, Cell line, Chemical synthesis, Chemotherapy, Cytotoxicity, Fetus, Human, In vitro, In vivo, Lung, Malaria, Mouse, Nitrogen heterocycle, Oral administration, Organic carbamate, Parasiticide, Plasmodium berghei, Plasmodium falciparum, Quinoline derivatives, Six membered ring, Structure activity relation, Toxicity.

Abstract

A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

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A02	`01`			`@0 EJMCA5`
A03		`1`		`@0 Eur. j. med. chem.`
A05				`@2 43`
A06				`@2 10`
A08	`01`	`1`	`ENG`	`@1 Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline`
A11	`01`	`1`		`@1 DELARUE-COCHIN (Sandrine)`
A11	`02`	`1`		`@1 GRELLIER (Philippe)`
A11	`03`	`1`		`@1 MAES (Louis)`
A11	`04`	`1`		`@1 MOURAY (Elisabeth)`
A11	`05`	`1`		`@1 SERGHERAERT (Christian)`
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A14	`02`			`@1 USM504-EA3335, Département RDDM, CP52, Muséum National d'Histoire Naturelle, 61 rue Buffon @2 75005 Paris @3 FRA @Z 2 aut. @Z 4 aut.`
A14	`03`			`@1 Tibotec @2 32800 Mechelen @3 BEL @Z 3 aut.`
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A20				`@1 2045-2055`
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A44				`@0 0000 @1 © 2008 INIST-CNRS. All rights reserved.`
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C01	`01`		`ENG`	@0 A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.
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C03	`01`	`X`	`ENG`	`@0 Chemical synthesis @5 01`
C03	`01`	`X`	`SPA`	`@0 Síntesis química @5 01`
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C03	`03`	`X`	`FRE`	`@0 Relation structure activité @5 03`
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C03	`04`	`X`	`FRE`	`@0 Carbamate organique @5 04`
C03	`04`	`X`	`ENG`	`@0 Organic carbamate @5 04`
C03	`04`	`X`	`SPA`	`@0 Carbamato orgánico @5 04`
C03	`05`	`X`	`FRE`	`@0 Carboxamide @5 05`
C03	`05`	`X`	`ENG`	`@0 Carboxamide @5 05`
C03	`05`	`X`	`SPA`	`@0 Carboxamida @5 05`
C03	`06`	`X`	`FRE`	`@0 Dérivé de l'aniline @5 06`
C03	`06`	`X`	`ENG`	`@0 Aniline derivatives @5 06`
C03	`06`	`X`	`SPA`	`@0 Anilina derivado @5 06`
C03	`07`	`X`	`FRE`	`@0 Dérivé de la quinoléine @2 FF @5 07`
C03	`07`	`X`	`ENG`	`@0 Quinoline derivatives @2 FF @5 07`
C03	`07`	`X`	`SPA`	`@0 Quinolina derivado @2 FF @5 07`
C03	`08`	`X`	`FRE`	`@0 Plasmodium falciparum @2 NS @5 09`
C03	`08`	`X`	`ENG`	`@0 Plasmodium falciparum @2 NS @5 09`
C03	`08`	`X`	`SPA`	`@0 Plasmodium falciparum @2 NS @5 09`
C03	`09`	`X`	`FRE`	`@0 Amodiaquine @2 NK @2 FR @5 10`
C03	`09`	`X`	`ENG`	`@0 Amodiaquine @2 NK @2 FR @5 10`
C03	`09`	`X`	`SPA`	`@0 Amodiaquina @2 NK @2 FR @5 10`
C03	`10`	`X`	`FRE`	`@0 Hétérocycle azote @5 11`
C03	`10`	`X`	`ENG`	`@0 Nitrogen heterocycle @5 11`
C03	`10`	`X`	`SPA`	`@0 Heterociclo nitrógeno @5 11`
C03	`11`	`X`	`FRE`	`@0 Dérivé du benzène @5 12`
C03	`11`	`X`	`ENG`	`@0 Benzene derivatives @5 12`
C03	`11`	`X`	`SPA`	`@0 Benceno derivado @5 12`
C03	`12`	`X`	`FRE`	`@0 Composé bicyclique @5 13`
C03	`12`	`X`	`ENG`	`@0 Bicyclic compound @5 13`
C03	`12`	`X`	`SPA`	`@0 Compuesto bicíclico @5 13`
C03	`13`	`X`	`FRE`	`@0 Cycle 6 chaînons @5 14`
C03	`13`	`X`	`ENG`	`@0 Six membered ring @5 14`
C03	`13`	`X`	`SPA`	`@0 Ciclo 6 eslabones @5 14`
C03	`14`	`X`	`FRE`	`@0 In vitro @5 15`
C03	`14`	`X`	`ENG`	`@0 In vitro @5 15`
C03	`14`	`X`	`SPA`	`@0 In vitro @5 15`
C03	`15`	`X`	`FRE`	`@0 In vivo @5 16`
C03	`15`	`X`	`ENG`	`@0 In vivo @5 16`
C03	`15`	`X`	`SPA`	`@0 In vivo @5 16`
C03	`16`	`X`	`FRE`	`@0 Chimiothérapie @5 17`
C03	`16`	`X`	`ENG`	`@0 Chemotherapy @5 17`
C03	`16`	`X`	`SPA`	`@0 Quimioterapia @5 17`
C03	`17`	`X`	`FRE`	`@0 Plasmodium berghei @2 NS @5 19`
C03	`17`	`X`	`ENG`	`@0 Plasmodium berghei @2 NS @5 19`
C03	`17`	`X`	`SPA`	`@0 Plasmodium berghei @2 NS @5 19`
C03	`18`	`X`	`FRE`	`@0 Toxicité @5 20`
C03	`18`	`X`	`ENG`	`@0 Toxicity @5 20`
C03	`18`	`X`	`SPA`	`@0 Toxicidad @5 20`
C03	`19`	`X`	`FRE`	`@0 Cytotoxicité @5 21`
C03	`19`	`X`	`ENG`	`@0 Cytotoxicity @5 21`
C03	`19`	`X`	`SPA`	`@0 Citotoxicidad @5 21`
C03	`20`	`X`	`FRE`	`@0 Composé aromatique @5 22`
C03	`20`	`X`	`ENG`	`@0 Aromatic compound @5 22`
C03	`20`	`X`	`SPA`	`@0 Compuesto aromático @5 22`
C03	`21`	`X`	`FRE`	`@0 Voie orale @5 23`
C03	`21`	`X`	`ENG`	`@0 Oral administration @5 23`
C03	`21`	`X`	`SPA`	`@0 Vía oral @5 23`
C03	`22`	`X`	`FRE`	`@0 Paludisme @5 24`
C03	`22`	`X`	`ENG`	`@0 Malaria @5 24`
C03	`22`	`X`	`SPA`	`@0 Paludismo @5 24`
C03	`23`	`X`	`FRE`	`@0 Souris @5 25`
C03	`23`	`X`	`ENG`	`@0 Mouse @5 25`
C03	`23`	`X`	`SPA`	`@0 Ratón @5 25`
C03	`24`	`X`	`FRE`	`@0 Antiparasitaire @5 32`
C03	`24`	`X`	`ENG`	`@0 Parasiticide @5 32`
C03	`24`	`X`	`SPA`	`@0 Antiparasitario @5 32`
C03	`25`	`X`	`FRE`	`@0 Antiprotozoaire @5 33`
C03	`25`	`X`	`ENG`	`@0 Antiprotozoal agent @5 33`
C03	`25`	`X`	`SPA`	`@0 Antiprotozoario @5 33`
C03	`26`	`X`	`FRE`	`@0 Amine aromatique @5 34`
C03	`26`	`X`	`ENG`	`@0 Aromatic amine @5 34`
C03	`26`	`X`	`SPA`	`@0 Amina aromática @5 34`
C03	`27`	`X`	`FRE`	`@0 Foetus @5 35`
C03	`27`	`X`	`ENG`	`@0 Fetus @5 35`
C03	`27`	`X`	`SPA`	`@0 Feto @5 35`
C03	`28`	`X`	`FRE`	`@0 Poumon @5 36`
C03	`28`	`X`	`ENG`	`@0 Lung @5 36`
C03	`28`	`X`	`SPA`	`@0 Pulmón @5 36`
C03	`29`	`X`	`FRE`	`@0 Homme @5 37`
C03	`29`	`X`	`ENG`	`@0 Human @5 37`
C03	`29`	`X`	`SPA`	`@0 Hombre @5 37`
C03	`30`	`X`	`FRE`	`@0 Lignée cellulaire @5 38`
C03	`30`	`X`	`ENG`	`@0 Cell line @5 38`
C03	`30`	`X`	`SPA`	`@0 Línea celular @5 38`
C03	`31`	`X`	`FRE`	`@0 Animal @5 39`
C03	`31`	`X`	`ENG`	`@0 Animal @5 39`
C03	`31`	`X`	`SPA`	`@0 Animal @5 39`
C03	`32`	`X`	`FRE`	`@0 Pipéridine-1-acétamide dérivé @2 NK @4 INC @5 76`
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C07	`04`	`X`	`ENG`	`@0 Treatment`
C07	`04`	`X`	`SPA`	`@0 Tratamiento`
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C07	`05`	`X`	`ENG`	`@0 Protozoal disease`
C07	`05`	`X`	`SPA`	`@0 Protozoosis`
C07	`06`	`X`	`FRE`	`@0 Parasitose`
C07	`06`	`X`	`ENG`	`@0 Parasitosis`
C07	`06`	`X`	`SPA`	`@0 Parasitosis`
C07	`07`	`X`	`FRE`	`@0 Infection`
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C07	`07`	`X`	`SPA`	`@0 Infección`
C07	`08`	`X`	`FRE`	`@0 Rodentia @2 NS`
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C07	`08`	`X`	`SPA`	`@0 Rodentia @2 NS`
C07	`09`	`X`	`FRE`	`@0 Mammalia @2 NS`
C07	`09`	`X`	`ENG`	`@0 Mammalia @2 NS`
C07	`09`	`X`	`SPA`	`@0 Mammalia @2 NS`
C07	`10`	`X`	`FRE`	`@0 Vertebrata @2 NS`
C07	`10`	`X`	`ENG`	`@0 Vertebrata @2 NS`
C07	`10`	`X`	`SPA`	`@0 Vertebrata @2 NS`
N21				`@1 350`

Format Inist (serveur)

NO :	PASCAL 08-0535287 INIST
ET :	Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline
AU :	DELARUE-COCHIN (Sandrine); GRELLIER (Philippe); MAES (Louis); MOURAY (Elisabeth); SERGHERAERT (Christian); MELNYK (Patricia)
AF :	UMR CNRS 8525, Université de Lille 11, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447/59021 Lille/France (1 aut., 5 aut., 6 aut.); USM504-EA3335, Département RDDM, CP52, Muséum National d'Histoire Naturelle, 61 rue Buffon/75005 Paris/France (2 aut., 4 aut.); Tibotec/32800 Mechelen/Belgique (3 aut.); UMR CNRS 8161, Universités de Lille 1 & II, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447/59021 Lille/France (6 aut.)
DT :	Publication en série; Niveau analytique
SO :	European journal of medicinal chemistry; ISSN 0223-5234; Coden EJMCA5; Royaume-Uni; Da. 2008; Vol. 43; No. 10; Pp. 2045-2055; Bibl. 22 ref.
LA :	Anglais
EA :	A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.
CC :	002B02S06
FD :	Synthèse chimique; Antipaludique; Relation structure activité; Carbamate organique; Carboxamide; Dérivé de l'aniline; Dérivé de la quinoléine; Plasmodium falciparum; Amodiaquine; Hétérocycle azote; Dérivé du benzène; Composé bicyclique; Cycle 6 chaînons; In vitro; In vivo; Chimiothérapie; Plasmodium berghei; Toxicité; Cytotoxicité; Composé aromatique; Voie orale; Paludisme; Souris; Antiparasitaire; Antiprotozoaire; Amine aromatique; Foetus; Poumon; Homme; Lignée cellulaire; Animal; Pipéridine-1-acétamide dérivé; Lignée MRC5
FG :	Chlore Composé organique; Apicomplexa; Protozoa; Traitement; Protozoose; Parasitose; Infection; Rodentia; Mammalia; Vertebrata
ED :	Chemical synthesis; Antimalarial; Structure activity relation; Organic carbamate; Carboxamide; Aniline derivatives; Quinoline derivatives; Plasmodium falciparum; Amodiaquine; Nitrogen heterocycle; Benzene derivatives; Bicyclic compound; Six membered ring; In vitro; In vivo; Chemotherapy; Plasmodium berghei; Toxicity; Cytotoxicity; Aromatic compound; Oral administration; Malaria; Mouse; Parasiticide; Antiprotozoal agent; Aromatic amine; Fetus; Lung; Human; Cell line; Animal
EG :	Chlorine Organic compounds; Apicomplexa; Protozoa; Treatment; Protozoal disease; Parasitosis; Infection; Rodentia; Mammalia; Vertebrata
SD :	Síntesis química; Antipalúdico; Relación estructura actividad; Carbamato orgánico; Carboxamida; Anilina derivado; Quinolina derivado; Plasmodium falciparum; Amodiaquina; Heterociclo nitrógeno; Benceno derivado; Compuesto bicíclico; Ciclo 6 eslabones; In vitro; In vivo; Quimioterapia; Plasmodium berghei; Toxicidad; Citotoxicidad; Compuesto aromático; Vía oral; Paludismo; Ratón; Antiparasitario; Antiprotozoario; Amina aromática; Feto; Pulmón; Hombre; Línea celular; Animal
LO :	INIST-12640.354000183861600010
ID :	08-0535287

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Pascal:08-0535287

Le document en format XML

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<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Maes, Louis" sort="Maes, Louis" uniqKey="Maes L" first="Louis" last="Maes">Louis Maes</name>
<affiliation><inist:fA14 i1="03"><s1>Tibotec</s1>
<s2>32800 Mechelen</s2>
<s3>BEL</s3>
<sZ>3 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Mouray, Elisabeth" sort="Mouray, Elisabeth" uniqKey="Mouray E" first="Elisabeth" last="Mouray">Elisabeth Mouray</name>
<affiliation><inist:fA14 i1="02"><s1>USM504-EA3335, Département RDDM, CP52, Muséum National d'Histoire Naturelle, 61 rue Buffon</s1>
<s2>75005 Paris</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Sergheraert, Christian" sort="Sergheraert, Christian" uniqKey="Sergheraert C" first="Christian" last="Sergheraert">Christian Sergheraert</name>
<affiliation><inist:fA14 i1="01"><s1>UMR CNRS 8525, Université de Lille 11, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447</s1>
<s2>59021 Lille</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Melnyk, Patricia" sort="Melnyk, Patricia" uniqKey="Melnyk P" first="Patricia" last="Melnyk">Patricia Melnyk</name>
<affiliation><inist:fA14 i1="01"><s1>UMR CNRS 8525, Université de Lille 11, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447</s1>
<s2>59021 Lille</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="04"><s1>UMR CNRS 8161, Universités de Lille 1 & II, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447</s1>
<s2>59021 Lille</s2>
<s3>FRA</s3>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">European journal of medicinal chemistry</title>
<title level="j" type="abbreviated">Eur. j. med. chem.</title>
<idno type="ISSN">0223-5234</idno>
<imprint><date when="2008">2008</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><title level="j" type="main">European journal of medicinal chemistry</title>
<title level="j" type="abbreviated">Eur. j. med. chem.</title>
<idno type="ISSN">0223-5234</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Amodiaquine</term>
<term>Aniline derivatives</term>
<term>Animal</term>
<term>Antimalarial</term>
<term>Antiprotozoal agent</term>
<term>Aromatic amine</term>
<term>Aromatic compound</term>
<term>Benzene derivatives</term>
<term>Bicyclic compound</term>
<term>Carboxamide</term>
<term>Cell line</term>
<term>Chemical synthesis</term>
<term>Chemotherapy</term>
<term>Cytotoxicity</term>
<term>Fetus</term>
<term>Human</term>
<term>In vitro</term>
<term>In vivo</term>
<term>Lung</term>
<term>Malaria</term>
<term>Mouse</term>
<term>Nitrogen heterocycle</term>
<term>Oral administration</term>
<term>Organic carbamate</term>
<term>Parasiticide</term>
<term>Plasmodium berghei</term>
<term>Plasmodium falciparum</term>
<term>Quinoline derivatives</term>
<term>Six membered ring</term>
<term>Structure activity relation</term>
<term>Toxicity</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Synthèse chimique</term>
<term>Antipaludique</term>
<term>Relation structure activité</term>
<term>Carbamate organique</term>
<term>Carboxamide</term>
<term>Dérivé de l'aniline</term>
<term>Dérivé de la quinoléine</term>
<term>Plasmodium falciparum</term>
<term>Amodiaquine</term>
<term>Hétérocycle azote</term>
<term>Dérivé du benzène</term>
<term>Composé bicyclique</term>
<term>Cycle 6 chaînons</term>
<term>In vitro</term>
<term>In vivo</term>
<term>Chimiothérapie</term>
<term>Plasmodium berghei</term>
<term>Toxicité</term>
<term>Cytotoxicité</term>
<term>Composé aromatique</term>
<term>Voie orale</term>
<term>Paludisme</term>
<term>Souris</term>
<term>Antiparasitaire</term>
<term>Antiprotozoaire</term>
<term>Amine aromatique</term>
<term>Foetus</term>
<term>Poumon</term>
<term>Homme</term>
<term>Lignée cellulaire</term>
<term>Animal</term>
<term>Pipéridine-1-acétamide dérivé</term>
<term>Lignée MRC5</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.</div>
</front>
</TEI>
<inist><standard h6="B"><pA><fA01 i1="01" i2="1"><s0>0223-5234</s0>
</fA01>
<fA02 i1="01"><s0>EJMCA5</s0>
</fA02>
<fA03 i2="1"><s0>Eur. j. med. chem.</s0>
</fA03>
<fA05><s2>43</s2>
</fA05>
<fA06><s2>10</s2>
</fA06>
<fA08 i1="01" i2="1" l="ENG"><s1>Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline</s1>
</fA08>
<fA11 i1="01" i2="1"><s1>DELARUE-COCHIN (Sandrine)</s1>
</fA11>
<fA11 i1="02" i2="1"><s1>GRELLIER (Philippe)</s1>
</fA11>
<fA11 i1="03" i2="1"><s1>MAES (Louis)</s1>
</fA11>
<fA11 i1="04" i2="1"><s1>MOURAY (Elisabeth)</s1>
</fA11>
<fA11 i1="05" i2="1"><s1>SERGHERAERT (Christian)</s1>
</fA11>
<fA11 i1="06" i2="1"><s1>MELNYK (Patricia)</s1>
</fA11>
<fA14 i1="01"><s1>UMR CNRS 8525, Université de Lille 11, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447</s1>
<s2>59021 Lille</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</fA14>
<fA14 i1="02"><s1>USM504-EA3335, Département RDDM, CP52, Muséum National d'Histoire Naturelle, 61 rue Buffon</s1>
<s2>75005 Paris</s2>
<s3>FRA</s3>
<sZ>2 aut.</sZ>
<sZ>4 aut.</sZ>
</fA14>
<fA14 i1="03"><s1>Tibotec</s1>
<s2>32800 Mechelen</s2>
<s3>BEL</s3>
<sZ>3 aut.</sZ>
</fA14>
<fA14 i1="04"><s1>UMR CNRS 8161, Universités de Lille 1 & II, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447</s1>
<s2>59021 Lille</s2>
<s3>FRA</s3>
<sZ>6 aut.</sZ>
</fA14>
<fA20><s1>2045-2055</s1>
</fA20>
<fA21><s1>2008</s1>
</fA21>
<fA23 i1="01"><s0>ENG</s0>
</fA23>
<fA43 i1="01"><s1>INIST</s1>
<s2>12640</s2>
<s5>354000183861600010</s5>
</fA43>
<fA44><s0>0000</s0>
<s1>© 2008 INIST-CNRS. All rights reserved.</s1>
</fA44>
<fA45><s0>22 ref.</s0>
</fA45>
<fA47 i1="01" i2="1"><s0>08-0535287</s0>
</fA47>
<fA60><s1>P</s1>
</fA60>
<fA61><s0>A</s0>
</fA61>
<fA64 i1="01" i2="1"><s0>European journal of medicinal chemistry</s0>
</fA64>
<fA66 i1="01"><s0>GBR</s0>
</fA66>
<fC01 i1="01" l="ENG"><s0>A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.</s0>
</fC01>
<fC02 i1="01" i2="X"><s0>002B02S06</s0>
</fC02>
<fC03 i1="01" i2="X" l="FRE"><s0>Synthèse chimique</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="ENG"><s0>Chemical synthesis</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="SPA"><s0>Síntesis química</s0>
<s5>01</s5>
</fC03>
<fC03 i1="02" i2="X" l="FRE"><s0>Antipaludique</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="ENG"><s0>Antimalarial</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="SPA"><s0>Antipalúdico</s0>
<s5>02</s5>
</fC03>
<fC03 i1="03" i2="X" l="FRE"><s0>Relation structure activité</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="ENG"><s0>Structure activity relation</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="SPA"><s0>Relación estructura actividad</s0>
<s5>03</s5>
</fC03>
<fC03 i1="04" i2="X" l="FRE"><s0>Carbamate organique</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="ENG"><s0>Organic carbamate</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="SPA"><s0>Carbamato orgánico</s0>
<s5>04</s5>
</fC03>
<fC03 i1="05" i2="X" l="FRE"><s0>Carboxamide</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="ENG"><s0>Carboxamide</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="SPA"><s0>Carboxamida</s0>
<s5>05</s5>
</fC03>
<fC03 i1="06" i2="X" l="FRE"><s0>Dérivé de l'aniline</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG"><s0>Aniline derivatives</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="SPA"><s0>Anilina derivado</s0>
<s5>06</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE"><s0>Dérivé de la quinoléine</s0>
<s2>FF</s2>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG"><s0>Quinoline derivatives</s0>
<s2>FF</s2>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA"><s0>Quinolina derivado</s0>
<s2>FF</s2>
<s5>07</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE"><s0>Plasmodium falciparum</s0>
<s2>NS</s2>
<s5>09</s5>
</fC03>
<fC03 i1="08" i2="X" l="ENG"><s0>Plasmodium falciparum</s0>
<s2>NS</s2>
<s5>09</s5>
</fC03>
<fC03 i1="08" i2="X" l="SPA"><s0>Plasmodium falciparum</s0>
<s2>NS</s2>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="FRE"><s0>Amodiaquine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>10</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG"><s0>Amodiaquine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>10</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA"><s0>Amodiaquina</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE"><s0>Hétérocycle azote</s0>
<s5>11</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG"><s0>Nitrogen heterocycle</s0>
<s5>11</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA"><s0>Heterociclo nitrógeno</s0>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="FRE"><s0>Dérivé du benzène</s0>
<s5>12</s5>
</fC03>
<fC03 i1="11" i2="X" l="ENG"><s0>Benzene derivatives</s0>
<s5>12</s5>
</fC03>
<fC03 i1="11" i2="X" l="SPA"><s0>Benceno derivado</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="FRE"><s0>Composé bicyclique</s0>
<s5>13</s5>
</fC03>
<fC03 i1="12" i2="X" l="ENG"><s0>Bicyclic compound</s0>
<s5>13</s5>
</fC03>
<fC03 i1="12" i2="X" l="SPA"><s0>Compuesto bicíclico</s0>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="FRE"><s0>Cycle 6 chaînons</s0>
<s5>14</s5>
</fC03>
<fC03 i1="13" i2="X" l="ENG"><s0>Six membered ring</s0>
<s5>14</s5>
</fC03>
<fC03 i1="13" i2="X" l="SPA"><s0>Ciclo 6 eslabones</s0>
<s5>14</s5>
</fC03>
<fC03 i1="14" i2="X" l="FRE"><s0>In vitro</s0>
<s5>15</s5>
</fC03>
<fC03 i1="14" i2="X" l="ENG"><s0>In vitro</s0>
<s5>15</s5>
</fC03>
<fC03 i1="14" i2="X" l="SPA"><s0>In vitro</s0>
<s5>15</s5>
</fC03>
<fC03 i1="15" i2="X" l="FRE"><s0>In vivo</s0>
<s5>16</s5>
</fC03>
<fC03 i1="15" i2="X" l="ENG"><s0>In vivo</s0>
<s5>16</s5>
</fC03>
<fC03 i1="15" i2="X" l="SPA"><s0>In vivo</s0>
<s5>16</s5>
</fC03>
<fC03 i1="16" i2="X" l="FRE"><s0>Chimiothérapie</s0>
<s5>17</s5>
</fC03>
<fC03 i1="16" i2="X" l="ENG"><s0>Chemotherapy</s0>
<s5>17</s5>
</fC03>
<fC03 i1="16" i2="X" l="SPA"><s0>Quimioterapia</s0>
<s5>17</s5>
</fC03>
<fC03 i1="17" i2="X" l="FRE"><s0>Plasmodium berghei</s0>
<s2>NS</s2>
<s5>19</s5>
</fC03>
<fC03 i1="17" i2="X" l="ENG"><s0>Plasmodium berghei</s0>
<s2>NS</s2>
<s5>19</s5>
</fC03>
<fC03 i1="17" i2="X" l="SPA"><s0>Plasmodium berghei</s0>
<s2>NS</s2>
<s5>19</s5>
</fC03>
<fC03 i1="18" i2="X" l="FRE"><s0>Toxicité</s0>
<s5>20</s5>
</fC03>
<fC03 i1="18" i2="X" l="ENG"><s0>Toxicity</s0>
<s5>20</s5>
</fC03>
<fC03 i1="18" i2="X" l="SPA"><s0>Toxicidad</s0>
<s5>20</s5>
</fC03>
<fC03 i1="19" i2="X" l="FRE"><s0>Cytotoxicité</s0>
<s5>21</s5>
</fC03>
<fC03 i1="19" i2="X" l="ENG"><s0>Cytotoxicity</s0>
<s5>21</s5>
</fC03>
<fC03 i1="19" i2="X" l="SPA"><s0>Citotoxicidad</s0>
<s5>21</s5>
</fC03>
<fC03 i1="20" i2="X" l="FRE"><s0>Composé aromatique</s0>
<s5>22</s5>
</fC03>
<fC03 i1="20" i2="X" l="ENG"><s0>Aromatic compound</s0>
<s5>22</s5>
</fC03>
<fC03 i1="20" i2="X" l="SPA"><s0>Compuesto aromático</s0>
<s5>22</s5>
</fC03>
<fC03 i1="21" i2="X" l="FRE"><s0>Voie orale</s0>
<s5>23</s5>
</fC03>
<fC03 i1="21" i2="X" l="ENG"><s0>Oral administration</s0>
<s5>23</s5>
</fC03>
<fC03 i1="21" i2="X" l="SPA"><s0>Vía oral</s0>
<s5>23</s5>
</fC03>
<fC03 i1="22" i2="X" l="FRE"><s0>Paludisme</s0>
<s5>24</s5>
</fC03>
<fC03 i1="22" i2="X" l="ENG"><s0>Malaria</s0>
<s5>24</s5>
</fC03>
<fC03 i1="22" i2="X" l="SPA"><s0>Paludismo</s0>
<s5>24</s5>
</fC03>
<fC03 i1="23" i2="X" l="FRE"><s0>Souris</s0>
<s5>25</s5>
</fC03>
<fC03 i1="23" i2="X" l="ENG"><s0>Mouse</s0>
<s5>25</s5>
</fC03>
<fC03 i1="23" i2="X" l="SPA"><s0>Ratón</s0>
<s5>25</s5>
</fC03>
<fC03 i1="24" i2="X" l="FRE"><s0>Antiparasitaire</s0>
<s5>32</s5>
</fC03>
<fC03 i1="24" i2="X" l="ENG"><s0>Parasiticide</s0>
<s5>32</s5>
</fC03>
<fC03 i1="24" i2="X" l="SPA"><s0>Antiparasitario</s0>
<s5>32</s5>
</fC03>
<fC03 i1="25" i2="X" l="FRE"><s0>Antiprotozoaire</s0>
<s5>33</s5>
</fC03>
<fC03 i1="25" i2="X" l="ENG"><s0>Antiprotozoal agent</s0>
<s5>33</s5>
</fC03>
<fC03 i1="25" i2="X" l="SPA"><s0>Antiprotozoario</s0>
<s5>33</s5>
</fC03>
<fC03 i1="26" i2="X" l="FRE"><s0>Amine aromatique</s0>
<s5>34</s5>
</fC03>
<fC03 i1="26" i2="X" l="ENG"><s0>Aromatic amine</s0>
<s5>34</s5>
</fC03>
<fC03 i1="26" i2="X" l="SPA"><s0>Amina aromática</s0>
<s5>34</s5>
</fC03>
<fC03 i1="27" i2="X" l="FRE"><s0>Foetus</s0>
<s5>35</s5>
</fC03>
<fC03 i1="27" i2="X" l="ENG"><s0>Fetus</s0>
<s5>35</s5>
</fC03>
<fC03 i1="27" i2="X" l="SPA"><s0>Feto</s0>
<s5>35</s5>
</fC03>
<fC03 i1="28" i2="X" l="FRE"><s0>Poumon</s0>
<s5>36</s5>
</fC03>
<fC03 i1="28" i2="X" l="ENG"><s0>Lung</s0>
<s5>36</s5>
</fC03>
<fC03 i1="28" i2="X" l="SPA"><s0>Pulmón</s0>
<s5>36</s5>
</fC03>
<fC03 i1="29" i2="X" l="FRE"><s0>Homme</s0>
<s5>37</s5>
</fC03>
<fC03 i1="29" i2="X" l="ENG"><s0>Human</s0>
<s5>37</s5>
</fC03>
<fC03 i1="29" i2="X" l="SPA"><s0>Hombre</s0>
<s5>37</s5>
</fC03>
<fC03 i1="30" i2="X" l="FRE"><s0>Lignée cellulaire</s0>
<s5>38</s5>
</fC03>
<fC03 i1="30" i2="X" l="ENG"><s0>Cell line</s0>
<s5>38</s5>
</fC03>
<fC03 i1="30" i2="X" l="SPA"><s0>Línea celular</s0>
<s5>38</s5>
</fC03>
<fC03 i1="31" i2="X" l="FRE"><s0>Animal</s0>
<s5>39</s5>
</fC03>
<fC03 i1="31" i2="X" l="ENG"><s0>Animal</s0>
<s5>39</s5>
</fC03>
<fC03 i1="31" i2="X" l="SPA"><s0>Animal</s0>
<s5>39</s5>
</fC03>
<fC03 i1="32" i2="X" l="FRE"><s0>Pipéridine-1-acétamide dérivé</s0>
<s2>NK</s2>
<s4>INC</s4>
<s5>76</s5>
</fC03>
<fC03 i1="33" i2="X" l="FRE"><s0>Lignée MRC5</s0>
<s4>INC</s4>
<s5>77</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE"><s0>Chlore Composé organique</s0>
<s2>NC</s2>
<s2>FX</s2>
<s2>NA</s2>
<s5>08</s5>
</fC07>
<fC07 i1="01" i2="X" l="ENG"><s0>Chlorine Organic compounds</s0>
<s2>NC</s2>
<s2>FX</s2>
<s2>NA</s2>
<s5>08</s5>
</fC07>
<fC07 i1="01" i2="X" l="SPA"><s0>Cloro Compuesto orgánico</s0>
<s2>NC</s2>
<s2>FX</s2>
<s2>NA</s2>
<s5>08</s5>
</fC07>
<fC07 i1="02" i2="X" l="FRE"><s0>Apicomplexa</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="ENG"><s0>Apicomplexa</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="SPA"><s0>Apicomplexa</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="FRE"><s0>Protozoa</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="ENG"><s0>Protozoa</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="SPA"><s0>Protozoa</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="04" i2="X" l="FRE"><s0>Traitement</s0>
</fC07>
<fC07 i1="04" i2="X" l="ENG"><s0>Treatment</s0>
</fC07>
<fC07 i1="04" i2="X" l="SPA"><s0>Tratamiento</s0>
</fC07>
<fC07 i1="05" i2="X" l="FRE"><s0>Protozoose</s0>
</fC07>
<fC07 i1="05" i2="X" l="ENG"><s0>Protozoal disease</s0>
</fC07>
<fC07 i1="05" i2="X" l="SPA"><s0>Protozoosis</s0>
</fC07>
<fC07 i1="06" i2="X" l="FRE"><s0>Parasitose</s0>
</fC07>
<fC07 i1="06" i2="X" l="ENG"><s0>Parasitosis</s0>
</fC07>
<fC07 i1="06" i2="X" l="SPA"><s0>Parasitosis</s0>
</fC07>
<fC07 i1="07" i2="X" l="FRE"><s0>Infection</s0>
</fC07>
<fC07 i1="07" i2="X" l="ENG"><s0>Infection</s0>
</fC07>
<fC07 i1="07" i2="X" l="SPA"><s0>Infección</s0>
</fC07>
<fC07 i1="08" i2="X" l="FRE"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="08" i2="X" l="ENG"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="08" i2="X" l="SPA"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="09" i2="X" l="FRE"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="09" i2="X" l="ENG"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="09" i2="X" l="SPA"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="10" i2="X" l="FRE"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="10" i2="X" l="ENG"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="10" i2="X" l="SPA"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fN21><s1>350</s1>
</fN21>
</pA>
</standard>
<server><NO>PASCAL 08-0535287 INIST</NO>
<ET>Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline</ET>
<AU>DELARUE-COCHIN (Sandrine); GRELLIER (Philippe); MAES (Louis); MOURAY (Elisabeth); SERGHERAERT (Christian); MELNYK (Patricia)</AU>
<AF>UMR CNRS 8525, Université de Lille 11, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447/59021 Lille/France (1 aut., 5 aut., 6 aut.); USM504-EA3335, Département RDDM, CP52, Muséum National d'Histoire Naturelle, 61 rue Buffon/75005 Paris/France (2 aut., 4 aut.); Tibotec/32800 Mechelen/Belgique (3 aut.); UMR CNRS 8161, Universités de Lille 1 & II, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447/59021 Lille/France (6 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>European journal of medicinal chemistry; ISSN 0223-5234; Coden EJMCA5; Royaume-Uni; Da. 2008; Vol. 43; No. 10; Pp. 2045-2055; Bibl. 22 ref.</SO>
<LA>Anglais</LA>
<EA>A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.</EA>
<CC>002B02S06</CC>
<FD>Synthèse chimique; Antipaludique; Relation structure activité; Carbamate organique; Carboxamide; Dérivé de l'aniline; Dérivé de la quinoléine; Plasmodium falciparum; Amodiaquine; Hétérocycle azote; Dérivé du benzène; Composé bicyclique; Cycle 6 chaînons; In vitro; In vivo; Chimiothérapie; Plasmodium berghei; Toxicité; Cytotoxicité; Composé aromatique; Voie orale; Paludisme; Souris; Antiparasitaire; Antiprotozoaire; Amine aromatique; Foetus; Poumon; Homme; Lignée cellulaire; Animal; Pipéridine-1-acétamide dérivé; Lignée MRC5</FD>
<FG>Chlore Composé organique; Apicomplexa; Protozoa; Traitement; Protozoose; Parasitose; Infection; Rodentia; Mammalia; Vertebrata</FG>
<ED>Chemical synthesis; Antimalarial; Structure activity relation; Organic carbamate; Carboxamide; Aniline derivatives; Quinoline derivatives; Plasmodium falciparum; Amodiaquine; Nitrogen heterocycle; Benzene derivatives; Bicyclic compound; Six membered ring; In vitro; In vivo; Chemotherapy; Plasmodium berghei; Toxicity; Cytotoxicity; Aromatic compound; Oral administration; Malaria; Mouse; Parasiticide; Antiprotozoal agent; Aromatic amine; Fetus; Lung; Human; Cell line; Animal</ED>
<EG>Chlorine Organic compounds; Apicomplexa; Protozoa; Treatment; Protozoal disease; Parasitosis; Infection; Rodentia; Mammalia; Vertebrata</EG>
<SD>Síntesis química; Antipalúdico; Relación estructura actividad; Carbamato orgánico; Carboxamida; Anilina derivado; Quinolina derivado; Plasmodium falciparum; Amodiaquina; Heterociclo nitrógeno; Benceno derivado; Compuesto bicíclico; Ciclo 6 eslabones; In vitro; In vivo; Quimioterapia; Plasmodium berghei; Toxicidad; Citotoxicidad; Compuesto aromático; Vía oral; Paludismo; Ratón; Antiparasitario; Antiprotozoario; Amina aromática; Feto; Pulmón; Hombre; Línea celular; Animal</SD>
<LO>INIST-12640.354000183861600010</LO>
<ID>08-0535287</ID>
</server>
</inist>
</record>

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Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline

Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline

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