Bioorganic and Medicinal Chemistry Letters p. 2891 - 2895 (2008)
Update date:2022-08-03
Topics:
De Luca, Laura
Barreca, Maria Letizia
Ferro, Stefania
Iraci, Nunzio
Michiels, Martine
Christ, Frauke
Debyser, Zeger
Witvrouw, Myriam
Chimirri, Alba
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.
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(2008)