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

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

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(20): 6072-6075.

DOI：10.1016/j.bmcl.2010.08.063

• AMPA receptor
• Positive allosteric modulators
• Ion channels
• SBDD

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.

• 出版日期2010-10-15