par Vandurm, Pierre;Guiguen, Allan 
;Cauvin, Christine;Georges, Benoît;Le Van, Kiet ;Michaux, Catherine;Cardona, Christelle ;Mbemba, Gladys;Mouscadet, Jean-François;Hevesi, László;Van Lint, Carine ;Wouters, Johan
Référence European journal of medicinal chemistry, 46, 5, page (1749-1756)
Publication Publié, 2011
;Cauvin, Christine;Georges, Benoît;Le Van, Kiet ;Michaux, Catherine;Cardona, Christelle ;Mbemba, Gladys;Mouscadet, Jean-François;Hevesi, László;Van Lint, Carine ;Wouters, Johan Référence European journal of medicinal chemistry, 46, 5, page (1749-1756)
Publication Publié, 2011
Article révisé par les pairs
| 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. |
