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

Jamieson, Craig and Basten, Stephanie and Campbell, Robert A. and Cumming, Iain A. and Gillen, Kevin J. and Gillespie, Jonathan and Kazemier, Bert and Kiczun, Michael and Lamont, Yvonne and Lyons, Amanda J. and Maclean, John K.F. and Moir, Elizabeth M. and Morrow, John A. and Papakosta, Marianthi and Rankovic, Zoran and Smith, Lynn (2010) A novel series of positive modulators of the AMPA receptor : discovery and structure based hit-to-lead studies. Bioorganic and Medicinal Chemistry Letters, 20 (19). pp. 5753-5756. ISSN 0960-894X

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    Abstract

    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.