Literature DB >> 22778815

Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Jose María Cid1, Guillaume Duvey, Philippe Cluzeau, Vanthea Nhem, Karim Macary, Alexandre Raux, Nicolas Poirier, Jessica Muller, Christelle Boléa, Terry Finn, Sonia Poli, Mark Epping-Jordan, Emilie Chamelot, Francis Derouet, Francoise Girard, Gregor J Macdonald, Juan Antonio Vega, Ana Isabel de Lucas, Encarnación Matesanz, Hilde Lavreysen, María Lourdes Linares, Daniel Oehlrich, Julen Oyarzábal, Gary Tresadern, Andrés A Trabanco, Jose Ignacio Andrés, Emmanuel Le Poul, Hassan Imogai, Robert Lutjens, Jean-Philippe Rocher.   

Abstract

A series of 1,5-disubstituted pyridones was identified as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor 2 (mGluR2) via high throughput screening (HTS). Subsequent SAR exploration led to the identification of several compounds with improved in vitro activity. Lead compound 8 was further profiled and found to attenuate the increase in PCP induced locomotor activity in mice.

Entities:  

Keywords:  PAM; allosteric; glutamate; mGluR2; metabotropic; modulators

Mesh：

Substances：

Year:  2010        PMID： 22778815      PMCID： PMC3368638          DOI： 10.1021/cn1000638

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  14 in total

1.  Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.

Authors:  Anthony B Pinkerton; Rowena V Cube; John H Hutchinson; Joyce K James; Michael F Gardner; Hervé Schaffhauser; Blake A Rowe; Lorrie P Daggett; Jean-Michel Vernier
Journal:  Bioorg Med Chem Lett       Date:  2004-12-06       Impact factor: 2.823

Review 2.  Metabotropic glutamate receptors as novel targets for anxiety and stress disorders.

Authors:  Chad J Swanson; Mark Bures; Michael P Johnson; Anni-Maija Linden; James A Monn; Darryle D Schoepp
Journal:  Nat Rev Drug Discov       Date:  2005-02       Impact factor: 84.694

Review 3.  Progress in the developement of positive allosteric modulators of the metabotropic glutamate receptor 2.

Authors:  A A Trabanco; J M Cid; H Lavreysen; G J Macdonald; G Tresadern
Journal:  Curr Med Chem       Date:  2011       Impact factor: 4.530

4.  3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.

Authors:  Edward J Brnardic; Mark E Fraley; Robert M Garbaccio; Mark E Layton; John M Sanders; Chris Culberson; Marlene A Jacobson; Brian C Magliaro; Pete H Hutson; Julie A O'Brien; Sarah L Huszar; Jason M Uslaner; Kerry L Fillgrove; Cuyue Tang; Yuhsin Kuo; Sylvie M Sur; George D Hartman
Journal:  Bioorg Med Chem Lett       Date:  2010-03-31       Impact factor: 2.823

5.  Blockade of phencyclidine-induced hyperlocomotion by olanzapine, clozapine and serotonin receptor subtype selective antagonists in mice.

Authors:  S D Gleason; H E Shannon
Journal:  Psychopharmacology (Berl)       Date:  1997-01       Impact factor: 4.530

6.  Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial.

Authors:  Sandeep T Patil; Lu Zhang; Ferenc Martenyi; Stephen L Lowe; Kimberley A Jackson; Boris V Andreev; Alla S Avedisova; Leonid M Bardenstein; Issak Y Gurovich; Margarita A Morozova; Sergey N Mosolov; Nikolai G Neznanov; Alexander M Reznik; Anatoly B Smulevich; Vladimir A Tochilov; Bryan G Johnson; James A Monn; Darryle D Schoepp
Journal:  Nat Med       Date:  2007-09-02       Impact factor: 53.440

7.  Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.

Authors:  Gary Tresadern; Jose María Cid; Gregor J Macdonald; Juan Antonio Vega; Ana Isabel de Lucas; Aránzazu García; Encarnación Matesanz; María Lourdes Linares; Daniel Oehlrich; Hilde Lavreysen; Ilse Biesmans; Andrés A Trabanco
Journal:  Bioorg Med Chem Lett       Date:  2009-11-10       Impact factor: 2.823

8.  Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.

Authors:  Anthony B Pinkerton; Rowena V Cube; John H Hutchinson; Blake A Rowe; Hervé Schaffhauser; Xiumin Zhao; Lorrie P Daggett; Jean-Michel Vernier
Journal:  Bioorg Med Chem Lett       Date:  2004-11-01       Impact factor: 2.823

9.  Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039).

Authors:  Matthew J Fell; Kjell A Svensson; Bryan G Johnson; Darryle D Schoepp
Journal:  J Pharmacol Exp Ther       Date:  2008-04-18       Impact factor: 4.030

Review 10.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Arthur Christopoulos; Craig W Lindsley
Journal:  Nat Rev Drug Discov       Date:  2009-01       Impact factor: 84.694
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  6 in total

1.  Special issue on the pharmacology and medicinal chemistry of allosteric modulators of metabotropic glutamate receptors (mGluRs).

Authors:  Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

Review 2.  Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

Authors:  Douglas J Sheffler; Anthony B Pinkerton; Russell Dahl; Athina Markou; Nicholas D P Cosford
Journal:  ACS Chem Neurosci       Date:  2011-04-12       Impact factor: 4.418

3.  Is there a path forward for mGlu(2) positive allosteric modulators for the treatment of schizophrenia?

Authors:  Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2013-02-20       Impact factor: 4.418

4.  In Silico Studies Targeting G-protein Coupled Receptors for Drug Research Against Parkinson's Disease.

Authors:  Agostinho Lemos; Rita Melo; Antonio Jose Preto; Jose Guilherme Almeida; Irina Sousa Moreira; Maria Natalia Dias Soeiro Cordeiro
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

5.  Molecular determinants of positive allosteric modulation of the human metabotropic glutamate receptor 2.

Authors:  A Farinha; H Lavreysen; L Peeters; B Russo; S Masure; A A Trabanco; J Cid; G Tresadern
Journal:  Br J Pharmacol       Date:  2015-02-27       Impact factor: 8.739

Review 6.  Recent advances in the medicinal chemistry of group II and group III mGlu receptors.

Authors:  Chaobin Jin; Shutao Ma
Journal:  Medchemcomm       Date:  2017-01-13       Impact factor: 3.597
  6 in total

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