Literature DB >> 24900224

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

Robert M Garbaccio1, Edward J Brnardic1, Mark E Fraley1, George D Hartman1, Pete H Hutson2, Julie A O'Brien3, Brian C Magliaro2, Jason M Uslaner4, Sarah L Huszar4, Kerry L Fillgrove5, James H Small5, Cuyue Tang5, Yuhsin Kuo5, Marlene A Jacobson2.   

Abstract

Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physical and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clinical antipsychotic treatments for schizophrenia.

Entities:  

Keywords:  GPCR; Oxazolobenzimidazoles; allosteric modulators; hyperlocomotion model; metabotropic glutamate 2 receptor; schizophrenia

Year:  2010        PMID： 24900224      PMCID： PMC4007895          DOI： 10.1021/ml100115a

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  25 in total

Review 1.  Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia.

Authors:  Mark E Fraley
Journal:  Expert Opin Ther Pat       Date:  2009-09       Impact factor: 6.674

2.  Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice.

Authors:  Ruggero Galici; Carrie K Jones; Kamondanai Hemstapat; Yi Nong; Nicholas G Echemendia; Lilly C Williams; Tomas de Paulis; P Jeffrey Conn
Journal:  J Pharmacol Exp Ther       Date:  2006-04-11       Impact factor: 4.030

3.  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

4.  A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

Authors:  Gene G Kinney; Julie A O'Brien; Wei Lemaire; Maryann Burno; Denise J Bickel; Michelle K Clements; Tsing-Bau Chen; David D Wisnoski; Craig W Lindsley; Philip R Tiller; Sheri Smith; Marlene A Jacobson; Cyrille Sur; Mark E Duggan; Douglas J Pettibone; P Jeffrey Conn; David L Williams
Journal:  J Pharmacol Exp Ther       Date:  2004-12-17       Impact factor: 4.030

5.  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

Review 6.  Schizophrenia, "Just the Facts": what we know in 2008 part 1: overview.

Authors:  Rajiv Tandon; Matcheri S Keshavan; Henry A Nasrallah
Journal:  Schizophr Res       Date:  2008-03       Impact factor: 4.939

7.  Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor.

Authors:  Anthony B Pinkerton; Jean-Michel Vernier; Hervé Schaffhauser; Blake A Rowe; Una C Campbell; Dana E Rodriguez; Daniel S Lorrain; Christopher S Baccei; Lorrie P Daggett; Linda J Bristow
Journal:  J Med Chem       Date:  2004-08-26       Impact factor: 7.446

Review 8.  Metabotropic glutamate receptors: potential drug targets for the treatment of schizophrenia.

Authors:  Laura E Chavez-Noriega; Hervé Schaffhauser; Una C Campbell
Journal:  Curr Drug Targets CNS Neurol Disord       Date:  2002-06

Review 9.  Schizophrenia, "just the facts" what we know in 2008. 2. Epidemiology and etiology.

Authors:  Rajiv Tandon; Matcheri S Keshavan; Henry A Nasrallah
Journal:  Schizophr Res       Date:  2008-06-02       Impact factor: 4.939

10.  The de facto US mental and addictive disorders service system. Epidemiologic catchment area prospective 1-year prevalence rates of disorders and services.

Authors:  D A Regier; W E Narrow; D S Rae; R W Manderscheid; B Z Locke; F K Goodwin
Journal:  Arch Gen Psychiatry       Date:  1993-02
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  6 in total

Review 1.  Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Authors:  Craig W Lindsley; Kyle A Emmitte; Corey R Hopkins; Thomas M Bridges; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn
Journal:  Chem Rev       Date:  2016-02-16       Impact factor: 60.622

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.  Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.

Authors:  Joseph E Pero; Michael A Rossi; Michael J Kelly; Hannah D G F Lehman; Mark E Layton; Robert M Garbaccio; Julie A O'Brien; Brian C Magliaro; Jason M Uslaner; Sarah L Huszar; Kerry L Fillgrove; Cuyue Tang; Yuhsin Kuo; Leo A Joyce; Edward C Sherer; Marlene A Jacobson
Journal:  ACS Med Chem Lett       Date:  2016-01-10       Impact factor: 4.345

5.  Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.

Authors:  Shyama Sidique; Raveendra-Panickar Dhanya; Douglas J Sheffler; Hilary Highfield Nickols; Li Yang; Russell Dahl; Arianna Mangravita-Novo; Layton H Smith; Manoranjan S D'Souza; Svetlana Semenova; P Jeffrey Conn; Athina Markou; Nicholas D P Cosford
Journal:  J Med Chem       Date:  2012-10-23       Impact factor: 7.446

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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