Literature DB >> 19854049

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

Andrew S Felts1, Sam A Saleh, Uyen Le, Alice L Rodriguez, C David Weaver, P Jeffrey Conn, Craig W Lindsley, Kyle A Emmitte.   

Abstract

A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of metabotropic glutamate receptor 5 (mGlu(5)). This Letter describes the SAR of this series and the profile of selected compounds in selectivity and radioligand binding assays.

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Year:  2009        PMID： 19854049      PMCID： PMC2801349          DOI： 10.1016/j.bmcl.2009.10.024

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


  36 in total

Review 1.  mGluR5 antagonists: discovery, characterization and drug development.

Authors:  Fabrizio Gasparini; Graeme Bilbe; Baltazar Gomez-Mancilla; Will Spooren
Journal:  Curr Opin Drug Discov Devel       Date:  2008-09

2.  Knockdown of spinal metabotropic glutamate receptor 1 (mGluR(1)) alleviates pain and restores opioid efficacy after nerve injury in rats.

Authors:  M E Fundytus; K Yashpal; J G Chabot; M G Osborne; C D Lefebvre; A Dray; J L Henry; T J Coderre
Journal:  Br J Pharmacol       Date:  2001-01       Impact factor: 8.739

3.  Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines.

Authors:  A Gazit; J Chen; H App; G McMahon; P Hirth; I Chen; A Levitzki
Journal:  Bioorg Med Chem       Date:  1996-08       Impact factor: 3.641

4.  Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats.

Authors:  Małgorzata Pietraszek; Ilia Sukhanov; Piotr Maciejak; Janusz Szyndler; Andreas Gravius; Aleksandra Wisłowska; Adam Płaźnik; Anton Y Bespalov; Wojciech Danysz
Journal:  Eur J Pharmacol       Date:  2005-04-19       Impact factor: 4.432

5.  The anxiolytic-like activity of AIDA (1-aminoindan-1,5-dicarboxylic acid), an mGLu 1 receptor antagonist.

Authors:  A Kłodzińska; E Tatarczyńska; K Stachowicz; E Chojnacka-Wójcik
Journal:  J Physiol Pharmacol       Date:  2004-03       Impact factor: 3.011

6.  Transient lower esophageal sphincter relaxations in dogs are inhibited by a metabotropic glutamate receptor 5 antagonist.

Authors:  Jörgen Jensen; Anders Lehmann; Anna Uvebrant; Anita Carlsson; Gunilla Jerndal; Karolina Nilsson; Claudine Frisby; L Ashley Blackshaw; Jan P Mattsson
Journal:  Eur J Pharmacol       Date:  2005-09-05       Impact factor: 4.432

7.  Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling.

Authors:  Aleksandra Klodzinska; Ewa Tatarczyńska; Ewa Chojnacka-Wójcik; Gabriel Nowak; Nicholas D P Cosford; Andrzej Pilc
Journal:  Neuropharmacology       Date:  2004-09       Impact factor: 5.250

8.  The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety.

Authors:  Chris S Busse; Jesse Brodkin; David Tattersall; Jeffery J Anderson; Noelle Warren; Lida Tehrani; Linda J Bristow; Mark A Varney; Nicholas D P Cosford
Journal:  Neuropsychopharmacology       Date:  2004-11       Impact factor: 7.853

9.  A pilot open label, single dose trial of fenobam in adults with fragile X syndrome.

Authors:  E Berry-Kravis; D Hessl; S Coffey; C Hervey; A Schneider; J Yuhas; J Hutchison; M Snape; M Tranfaglia; D V Nguyen; R Hagerman
Journal:  J Med Genet       Date:  2009-01-06       Impact factor: 6.318

10.  A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease.

Authors:  C Keywood; M Wakefield; J Tack
Journal:  Gut       Date:  2009-05-20       Impact factor: 23.059
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  12 in total

1.  3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.

Authors:  Andrew S Felts; Stacey R Lindsley; Jeffrey P Lamb; Alice L Rodriguez; Usha N Menon; Satyawan Jadhav; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2010-06-15       Impact factor: 2.823

2.  Recent advances in the design and development of novel negative allosteric modulators of mGlu(5).

Authors:  Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

3.  (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.

Authors:  Craig W Lindsley; Brittney S Bates; Usha N Menon; Satyawan B Jadhav; Alexander S Kane; Carrie K Jones; Alice L Rodriguez; P Jeffrey Conn; Christopher M Olsen; Danny G Winder; Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

4.  N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.

Authors:  Andrew S Felts; Alice L Rodriguez; Ryan D Morrison; Daryl F Venable; Anna L Blobaum; Frank W Byers; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2016-03-09       Impact factor: 2.823

5.  Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Authors:  Andrew S Felts; Alice L Rodriguez; Ryan D Morrison; Daryl F Venable; Jason T Manka; Brittney S Bates; Anna L Blobaum; Frank W Byers; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2013-09-10       Impact factor: 2.823

6.  Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Authors:  Brittney S Bates; Alice L Rodriguez; Andrew S Felts; Ryan D Morrison; Daryl F Venable; Anna L Blobaum; Frank W Byers; Kera P Lawson; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2014-06-11       Impact factor: 2.823

7.  Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.

Authors:  Russell J Amato; Andrew S Felts; Alice L Rodriguez; Daryl F Venable; Ryan D Morrison; Frank W Byers; J Scott Daniels; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Carrie K Jones; Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2013-05-29       Impact factor: 4.418

Review 8.  Fragile X syndrome: an update on developing treatment modalities.

Authors:  Aileen Healy; Roger Rush; Timothy Ocain
Journal:  ACS Chem Neurosci       Date:  2011-03-22       Impact factor: 4.418

9.  Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Authors:  Karen J Gregory; Meredith J Noetzel; Jerri M Rook; Paige N Vinson; Shaun R Stauffer; Alice L Rodriguez; Kyle A Emmitte; Ya Zhou; Aspen C Chun; Andrew S Felts; Brian A Chauder; Craig W Lindsley; Colleen M Niswender; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2012-08-03       Impact factor: 4.436

Review 10.  Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window.

Authors:  Yoan Mihov; Gregor Hasler
Journal:  Int J Neuropsychopharmacol       Date:  2016-07-05       Impact factor: 5.176
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