A novel series of positive modulators of the AMPA receptor: structure-based lead optimization

Craig Jamieson, Robert A. Campbell, Iain A. Cumming, Kevin J. Gillen, Jonathan Gillespie, Bert Kazemier, Michael Kiczun, Yvonne Lamont, Amanda J. Lyons, John K.F. Maclean, Frederic Martin, Elizabeth M. Moir, John A. Morrow, John Pantling, Zoran Rankovic, Lynn Smith

Research output: Contribution to journalArticle

23 Citations (Scopus)
276 Downloads (Pure)

Abstract

Starting from lead compound 1, we demonstrate how x-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity.
Original languageEnglish
Pages (from-to)6072-6075
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number20
DOIs
Publication statusPublished - 15 Oct 2010

Keywords

  • AMPA receptor
  • ion channels
  • positive allosteric modulators
  • SBDD

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