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

[img] Microsoft Word (BMCL2_jm2.doc)
BMCL2_jm2.doc
Accepted Author Manuscript
Download (4MB)

    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 ORCID logoORCID: https://orcid.org/0000-0002-6567-8272, 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 and Smith, Lynn;
    Item type:Article
    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:16 Nov 2020 01:41
    Related URLs:
    URI:https://strathprints.strath.ac.uk/id/eprint/27801
    Export data:
    CORE (COnnecting REpositories)