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  3. A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series

A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2891-5. doi: 10.1016/j.bmcl.2008.03.089.
Laura De Luca 1,  Maria Letizia Barreca,  Stefania Ferro,  Nunzio Iraci,  Martine Michiels,  Frauke Christ,  Zeger Debyser,  Myriam Witvrouw,  Alba Chimirri
Affiliations

Affiliation

  • 1 Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy.
PMID: 18417342 DOI: 10.1016/j.bmcl.2008.03.089
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.

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