Literature DB >> 20409708

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

Edward J Brnardic1, 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.   

Abstract

Hit to lead optimization of (5R)-5-hexyl-3-phenyl-1,3-oxazolidin-2-one as a positive allosteric modulator of mGluR2 is described. Improvements in potency and metabolic stability were achieved through SAR on both ends of the oxazolidinone. An optimized lead compound was found to be brain penetrant and active in a rat ketamine-induced hyperlocomotion model for antipsychotic activity. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20409708     DOI： 10.1016/j.bmcl.2010.03.089

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


  5 in total

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

Authors:  Jose María Cid; 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
Journal:  ACS Chem Neurosci       Date:  2010-08-23       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.  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

4.  Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.

Authors:  Robert M Garbaccio; Edward J Brnardic; Mark E Fraley; George D Hartman; Pete H Hutson; Julie A O'Brien; Brian C Magliaro; Jason M Uslaner; Sarah L Huszar; Kerry L Fillgrove; James H Small; Cuyue Tang; Yuhsin Kuo; Marlene A Jacobson
Journal:  ACS Med Chem Lett       Date:  2010-07-12       Impact factor: 4.345

5.  Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

Authors:  Raveendra-Panickar Dhanya; Shyama Sidique; Douglas J Sheffler; Hilary Highfield Nickols; Ananda Herath; Li Yang; Russell Dahl; Robert Ardecky; Svetlana Semenova; Athina Markou; P Jeffrey Conn; Nicholas D P Cosford
Journal:  J Med Chem       Date:  2010-12-14       Impact factor: 7.446
  5 in total

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