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

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

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(19): 5753-5756.

DOI：10.1016/j.bmcl.2010.07.138

• AMPA receptor
• Allosteric modulator
• SBDD
• Hit-to-lead

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.

• 出版日期2010-10-1