A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.

نویسندگان

  • Craig Jamieson
  • Stephanie Basten
  • Robert A Campbell
  • Iain A Cumming
  • Kevin J Gillen
  • Jonathan Gillespie
  • Bert Kazemier
  • Michael Kiczun
  • Yvonne Lamont
  • Amanda J Lyons
  • John K F Maclean
  • Elizabeth M Moir
  • John A Morrow
  • Marianthi Papakosta
  • Zoran Rankovic
  • Lynn Smith
چکیده

Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 20 19  شماره 

صفحات  -

تاریخ انتشار 2010