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Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity

hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorDASSONVILLE-KLIMPT, Alexandra
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorSCHNEIDER, J.
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorDAMIANI, Céline
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorTISNERAT, Camille
hal.structure.identifierVecteurs - Infections tropicales et méditerranéennes [VITROME]
dc.contributor.authorCOHEN, Anita
hal.structure.identifierVecteurs - Infections tropicales et méditerranéennes [VITROME]
dc.contributor.authorAZAS, Nadine
hal.structure.identifierInstitut de Chimie de la Matière Condensée de Bordeaux [ICMCB]
dc.contributor.authorMARCHIVIE, Mathieu
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorGUILLON, J
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorMULLIÉ, Catherine
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorAGNAMEY, P.
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorTOTET, Anne
hal.structure.identifierVecteurs - Infections tropicales et méditerranéennes [VITROME]
hal.structure.identifierInstitut de Recherche Biomédicale des Armées [Brétigny-sur-Orge] [IRBA]
hal.structure.identifierInstitut Hospitalier Universitaire Méditerranée Infection [IHU Marseille]
dc.contributor.authorDORMOI, Jérôme
hal.structure.identifierInstitut de Recherche Biomédicale des Armées [Brétigny-sur-Orge] [IRBA]
dc.contributor.authorTAUDON, Nicolas
hal.structure.identifierVecteurs - Infections tropicales et méditerranéennes [VITROME]
hal.structure.identifierInstitut de Recherche Biomédicale des Armées [Brétigny-sur-Orge] [IRBA]
hal.structure.identifierInstitut Hospitalier Universitaire Méditerranée Infection [IHU Marseille]
hal.structure.identifierCentre National de Référence du Paludisme [IRBA, Marseille] [CNRP]
dc.contributor.authorPRADINES, Bruno
hal.structure.identifierAgents infectieux, résistance et chimiothérapie - UR UPJV 4294 [AGIR ]
dc.contributor.authorSONNET, Pascal
dc.date.issued2022
dc.identifier.issn0223-5234
dc.description.abstractEnMalaria is the fifth most lethal parasitic infections in the world. Herein, five new series of aminoalcohol quinolines including fifty-two compounds were designed, synthesized and evaluated in vitro against Pf3D7 and PfW2 strains. Among them, fourteen displayed IC50 values below or near of 50.0 nM whatever the strain with selectivity index often superior to 100. 17b was found as a promising antimalarial candidate with IC50 values of 14.9 nM and 11.0 nM against respectively Pf3D7 and PfW2 and a selectivity index higher than 770 whatever the cell line is. Further experiments were achieved to confirm the safety and to establish the preliminary ADMET profile of compound 17b before the in vivo study performed on a mouse model of P. berghei ANKA infection. The overall data of this study allowed to establish new structure-activity relationships and the development of novel agents with improved pharmacokinetic properties
dc.language.isoen
dc.publisherElsevier
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/
dc.subject.enMalaria
dc.subject.enP. falciparum
dc.subject.enantimalarial drug resistance
dc.subject.enmefloquine analogs
dc.subject.enaminoalcohol quinolines
dc.subject.enMalaria
dc.title.enDesign, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity
dc.typeArticle de revue
dc.identifier.doi10.1016/j.ejmech.2021.113981
dc.subject.halChimie/Matériaux
bordeaux.journalEuropean Journal of Medicinal Chemistry
bordeaux.page113981 (26 p.)
bordeaux.volume228
bordeaux.peerReviewedoui
hal.identifierhal-03464917
hal.version1
hal.popularnon
hal.audienceInternationale
hal.origin.linkhttps://hal.archives-ouvertes.fr//hal-03464917v1
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