A novel series of positive modulators of the AMPA receptor : structure-based lead optimization
Jamieson, Craig 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 Martin, Frederic and Moir, Elizabeth M. and Morrow, John A. and Pantling, John and Rankovic, Zoran and Smith, Lynn (2010) A novel series of positive modulators of the AMPA receptor : structure-based lead optimization. Bioorganic and Medicinal Chemistry Letters, 20 (20). pp. 6072-6075. ISSN 0960-894X
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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.
Creators(s): |
Jamieson, Craig ![]() | Item type: | Article |
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ID code: | 27801 |
Keywords: | AMPA receptor, ion channels, positive allosteric modulators, SBDD, Chemistry, Biochemistry, Organic Chemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Molecular Biology, Clinical Biochemistry |
Subjects: | Science > Chemistry |
Department: | Faculty of Science > Pure and Applied Chemistry Faculty of Engineering > Electronic and Electrical Engineering |
Depositing user: | Ms Carol Khalaf |
Date deposited: | 11 May 2011 14:13 |
Last modified: | 05 Feb 2021 02:52 |
Related URLs: | |
URI: | https://strathprints.strath.ac.uk/id/eprint/27801 |
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