Scaffold hopping: Application to the discovery of novel GABAA receptor ligands

J. L. Falcó, G. Plasencia, I. Zamora, M. Piqué, M. González, A. Morató, J. I. Borrell, J. Teixidó, I. Buira, E. Méndez, J. Terencio, M. Príncep, A. Palomer, A. Guglietta

Research output: Indexed journal article Articlepeer-review

1 Citation (Scopus)


Scaffold Hopping has been applied to the discovery of novel GABA A receptor ligands. Thus, bioisosteric replacement of the bicyclic imidazo[1,2-a]pyridine central core of Zolpidem by different heterocycles has been studied. The study has been divided into four different parts: 1) Scaffold Hopping calculations by using Shop software, 2) synthesis in the laboratory of all different chemical series, following an unique synthetic strategy, 3) screening of the molecules and 4) comparison of the activities found to the Shop predictions. Using this approach different tricycles have been discovered, showing interesting biological profile.

Original languageEnglish
Pages (from-to)324-328
Number of pages5
Issue number529
Publication statusPublished - May 2007


  • GABA
  • Scaffold hopping
  • Shop
  • Sleep disorders
  • Zolpidem


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