Literature DB >> 22352782

Imidazo[1,2-a]pyridines: orally active positive allosteric modulators of the metabotropic glutamate 2 receptor.

Andrés A Trabanco1, Gary Tresadern, Gregor J Macdonald, Juan Antonio Vega, Ana Isabel de Lucas, Encarnación Matesanz, Aránzazu García, María Lourdes Linares, Sergio A Alonso de Diego, José Manuel Alonso, Daniel Oehlrich, Abdelah Ahnaou, Wilhelmus Drinkenburg, Claire Mackie, José Ignacio Andrés, Hilde Lavreysen, José María Cid.   

Abstract

Advanced leads of an imidazopyridine series of positive allosteric modulators of the metabotropic glutamate 2 (mGlu2) receptor are reported. The optimization of in vitro ADMET and in vivo pharmacokinetic properties led to the identification of 27o. With good potency and selectivity for the mGlu2 receptor, 27o affected sleep-wake architecture in rats after oral treatment, which we have previously shown to be indicative of mGlu2 receptor-mediated central activity.

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Year:  2012        PMID： 22352782     DOI： 10.1021/jm201561r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  10 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

2.  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

3.  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

4.  Suzuki-Miyaura cross-coupling of unprotected, nitrogen-rich heterocycles: substrate scope and mechanistic investigation.

Authors:  M Alexander Düfert; Kelvin L Billingsley; Stephen L Buchwald
Journal:  J Am Chem Soc       Date:  2013-08-16       Impact factor: 15.419

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

6.  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

7.  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

Review 8.  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

9.  Synthesis, study of antileishmanial and antitrypanosomal activity of imidazo pyridine fused triazole analogues.

Authors:  Adinarayana Nandikolla; Singireddi Srinivasarao; Banoth Karan Kumar; Sankaranarayanan Murugesan; Himanshu Aggarwal; Louise L Major; Terry K Smith; Kondapalli Venkata Gowri Chandra Sekhar
Journal:  RSC Adv       Date:  2020-10-19       Impact factor: 4.036

10.  Regiocontrolled microwave assisted bifunctionalization of 7,8-dihalogenated imidazo[1,2-a]pyridines: a one pot double-coupling approach.

Authors:  Emilie Marie; Sébastien Bouclé; Cécile Enguehard-Gueiffier; Alain Gueiffier
Journal:  Molecules       Date:  2012-09-06       Impact factor: 4.411
  10 in total

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