Synthesis, biological evaluation and molecular modeling studies of quinolonyl diketo acid derivatives: New structural insight into the HIV-1 integrase inhibition

Pierre Vandurm, Allan Guiguen, Christine Cauvin, Benoît Georges, Kiet Le Van, Catherine Michaux, Christelle Cardona, Gladys Mbemba, Jean Franois Mouscadet, Laszlo Hevesi, Carine Van Lint, Johan Wouters

Résultats de recherche: Contribution à un journal/une revueArticle

Résumé

New quinolonyl diketo acid compounds bearing various substituents at position 6 of the quinolone scaffold were designed and synthesized as potential HIV-1 integrase inhibitors. These new compounds were evaluated for their antiviral and anti-integrase activity and showed inhibitory potency similar to that of 6-bromide analog 2. Molecular modeling and docking studies were performed to rationalize these data and to provide a detailed understanding of the mechanism of inhibition for this class of compounds.

langue originaleAnglais
Pages (de - à)1749-1756
Nombre de pages8
journalEuropean Journal of Medicinal Chemistry
Volume46
Numéro de publication5
Les DOIs
Etat de la publicationPublié - 1 mai 2011

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