Author/Authors :
Laura De Luca، نويسنده , , Maria Letizia Barreca، نويسنده , , Stefania Ferro، نويسنده , , Nunzio Iraci، نويسنده , , Martine Michiels، نويسنده , , Frauke Christ، نويسنده , , Zeger Debyser، نويسنده , , Myriam Witvrouw، نويسنده , , Alba Chimirri، نويسنده ,
Abstract :
We report herein the development of a new three-dimensional pharmacophore model for HIV-1 integrase inhibitors which led to the discovery of some 4-[1-(4-fluorobenzyl)-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acids that are able to specifically inhibit the strand transfer step of integration at nanomolar concentration. The synthesis of the new designed molecules is also described.
Keywords :
integrase , HIV , DKAs , Pharmacophore model , Synthesis of indole derivatives
