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  • Title: A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
    Author: Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L.
    Journal: Bioorg Med Chem Lett; 2010 Oct 15; 20(20):6072-5. PubMed ID: 20817521.
    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.
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