Literature DB >> 20817521

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

Craig Jamieson1, Robert A Campbell, Iain A Cumming, Kevin J Gillen, Jonathan Gillespie, Bert Kazemier, Michael Kiczun, Yvonne Lamont, Amanda J Lyons, John K F Maclean, Frederic Martin, Elizabeth M Moir, John A Morrow, John Pantling, Zoran Rankovic, Lynn Smith.   

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.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20817521     DOI: 10.1016/j.bmcl.2010.08.063

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Rational Design of a Novel AMPA Receptor Modulator through a Hybridization Approach.

Authors:  Nicola Caldwell; Jonathan E Harms; Kathryn M Partin; Craig Jamieson
Journal:  ACS Med Chem Lett       Date:  2015-02-11       Impact factor: 4.345

2.  Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy.

Authors:  Jonathan E Harms; Morris Benveniste; John K F Maclean; Kathryn M Partin; Craig Jamieson
Journal:  Neuropharmacology       Date:  2012-06-23       Impact factor: 5.250

Review 3.  Structure and mechanism of glutamate receptor ion channel assembly, activation and modulation.

Authors:  Mark L Mayer
Journal:  Curr Opin Neurobiol       Date:  2011-02-23       Impact factor: 6.627

4.  Bivalent AMPA receptor positive allosteric modulators of the bis(pyrimidine) series.

Authors:  Anna A Nazarova; Kseniya N Sedenkova; Dmitry S Karlov; Mstislav I Lavrov; Yuri K Grishin; Tamara S Kuznetsova; Vladimir L Zamoyski; Vladimir V Grigoriev; Elena B Averina; Vladimir A Palyulin
Journal:  Medchemcomm       Date:  2019-07-12       Impact factor: 3.597

5.  Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.

Authors:  David E Timm; Morris Benveniste; Autumn M Weeks; Eric S Nisenbaum; Kathryn M Partin
Journal:  Mol Pharmacol       Date:  2011-05-04       Impact factor: 4.436

Review 6.  AMPA receptor potentiators: from drug design to cognitive enhancement.

Authors:  Kathryn M Partin
Journal:  Curr Opin Pharmacol       Date:  2014-11-27       Impact factor: 5.547

  6 in total

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