Arrêt de service programmé du vendredi 10 juin 16h jusqu’au lundi 13 juin 9h. Pour en savoir plus
Accéder directement au contenu Accéder directement à la navigation
Article dans une revue

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

Abstract : Malaria 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
Type de document :
Article dans une revue
Domaine :
Liste complète des métadonnées

https://hal.archives-ouvertes.fr/hal-03464917
Contributeur : Stéphane Toulin Connectez-vous pour contacter le contributeur
Soumis le : vendredi 3 décembre 2021 - 15:24:50
Dernière modification le : mercredi 16 mars 2022 - 15:32:03
Archivage à long terme le : : vendredi 4 mars 2022 - 19:14:53

Fichier

Dassonville-KlimptA_EurJMedChe...
Fichiers produits par l'(les) auteur(s)

Licence


Distributed under a Creative Commons Paternité - Pas d'utilisation commerciale - Pas de modification 4.0 International License

Identifiants

Citation

Alexandra Dassonville-Klimpt, J. Schneider, Céline Damiani, Camille Tisnerat, Anita Cohen, et al.. Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. European Journal of Medicinal Chemistry, Elsevier, 2022, 228, 113981 (26 p.). ⟨10.1016/j.ejmech.2021.113981⟩. ⟨hal-03464917⟩

Partager

Métriques

Consultations de la notice

62

Téléchargements de fichiers

2