Literature DB >> 20805031

A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.

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

Abstract

Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20805031     DOI: 10.1016/j.bmcl.2010.07.138

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


  7 in total

1.  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 2.  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

3.  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

Review 4.  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

5.  A one-pot synthesis 3-alkoxycarbonyl-3,4-dihydro-2H-pyran-2-ones from vinylidene melderum's acids, dialkyl acetylenedicarboxylates, and simple alcohols.

Authors:  Samira Khandan; Issa Yavari; Javad Azizian
Journal:  Mol Divers       Date:  2022-03-10       Impact factor: 2.943

6.  Exploiting drug-resistant enzymes as tools to identify thienopyrimidinone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.

Authors:  Takashi Masaoka; Suhman Chung; Pierluigi Caboni; Jason W Rausch; Jennifer A Wilson; Humeyra Taskent-Sezgin; John A Beutler; Graziella Tocco; Stuart F J Le Grice
Journal:  J Med Chem       Date:  2013-06-20       Impact factor: 7.446

Review 7.  Positive AMPA receptor modulation in the treatment of neuropsychiatric disorders: A long and winding road.

Authors:  Bashkim Kadriu; Laura Musazzi; Jenessa N Johnston; Lisa E Kalynchuk; Hector J Caruncho; Maurizio Popoli; Carlos A Zarate
Journal:  Drug Discov Today       Date:  2021-08-03       Impact factor: 8.369

  7 in total

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