1036765-52-2Relevant articles and documents
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series
De Luca, Laura,Barreca, Maria Letizia,Ferro, Stefania,Iraci, Nunzio,Michiels, Martine,Christ, Frauke,Debyser, Zeger,Witvrouw, Myriam,Chimirri, Alba
, p. 2891 - 2895 (2008)
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.