Literature DB >> 19932615

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

Gary Tresadern1, 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.   

Abstract

Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically stable compounds were found representing a promising avenue for current further studies. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 19932615     DOI： 10.1016/j.bmcl.2009.11.008

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


  16 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

2.  Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.

Authors:  Maarten L J Doornbos; Laura Pérez-Benito; Gary Tresadern; Thea Mulder-Krieger; Ilse Biesmans; Andrés A Trabanco; Jose María Cid; Hilde Lavreysen; Adriaan P IJzerman; Laura H Heitman
Journal:  Br J Pharmacol       Date:  2016-01-13       Impact factor: 8.739

Review 3.  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

4.  Molecular Scaffold Hopping via Holistic Molecular Representation.

Authors:  Francesca Grisoni; Gisbert Schneider
Journal:  Methods Mol Biol       Date:  2021

Review 5.  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

6.  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

7.  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

8.  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

9.  Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.

Authors:  Garrett C Moraski; Allen G Oliver; Lowell D Markley; Sanghyun Cho; Scott G Franzblau; Marvin J Miller
Journal:  Bioorg Med Chem Lett       Date:  2014-05-28       Impact factor: 2.823

10.  Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1H-benzimidazol-2-ones as mGlu2 Receptor PAMs.

Authors:  Ana Isabel de Lucas; Juan Antonio Vega; Encarnación Matesanz; María Lourdes Linares; Aránzazu García Molina; Gary Tresadern; Hilde Lavreysen; Andrés A Trabanco; José María Cid
Journal:  ACS Med Chem Lett       Date:  2019-10-10       Impact factor: 4.345
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