Literature DB >> 21779134

Preparation of a Series of 5-Methyl-3-(substituted)-[1,2,4]triazines.

Moses G Gichinga1, Jeremy P Olson, Elizabeth Butala, Brian P Gilmour, Hernán H Navarro, F Ivy Carroll.   

Abstract

Procedures for the synthesis of thirty-six 5-methyl-3-(substituted)-[1,2,4]triazines have been described. These compounds were evaluated for antagonism at metabotropic glutamate receptor subtype 5. Two compounds, 5b and 3c, were determined to be low micromolar inhibitors of mGluR5.

Entities:  

Year:  2011        PMID： 21779134      PMCID： PMC3138555          DOI： 10.1016/j.tetlet.2011.04.075

Source DB:  PubMed          Journal:  Tetrahedron Lett        ISSN： 0040-4039            Impact factor:   2.415


  7 in total

1.  Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice.

Authors:  C Chiamulera; M P Epping-Jordan; A Zocchi; C Marcon; C Cottiny; S Tacconi; M Corsi; F Orzi; F Conquet
Journal:  Nat Neurosci       Date:  2001-09       Impact factor: 24.884

2.  Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.

Authors:  Bernd Büttelmann; Jens-Uwe Peters; Simona Ceccarelli; Sabine Kolczewski; Eric Vieira; Eric P Prinssen; Will Spooren; Franz Schuler; Jörg Huwyler; Richard H P Porter; Georg Jaeschke
Journal:  Bioorg Med Chem Lett       Date:  2006-01-24       Impact factor: 2.823

3.  Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice.

Authors:  Xia Li; Anne B Need; Melvyn Baez; Jeffrey M Witkin
Journal:  J Pharmacol Exp Ther       Date:  2006-06-27       Impact factor: 4.030

Review 4.  Therapeutic implications of the mGluR theory of fragile X mental retardation.

Authors:  M F Bear
Journal:  Genes Brain Behav       Date:  2005-08       Impact factor: 3.449

5.  Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist.

Authors:  E Tatarczyńska; A Klodzińska; E Chojnacka-Wójcik; A Palucha; F Gasparini; R Kuhn; A Pilc
Journal:  Br J Pharmacol       Date:  2001-04       Impact factor: 8.739

6.  Up-regulation of metabotropic glutamate receptor subtypes 3 and 5 in spinal cord in a clinical model of persistent inflammation and hyperalgesia.

Authors:  Sharron Dolan; James G Kelly; Ana M Monteiro; Andrea M Nolan
Journal:  Pain       Date:  2003-12       Impact factor: 6.961

7.  Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.

Authors:  F Ivy Carroll; Sharadsrikar V Kotturi; Hernán A Navarro; S Wayne Mascarella; Brian P Gilmour; Forrest L Smith; Bichoy H Gabra; William L Dewey
Journal:  J Med Chem       Date:  2007-06-15       Impact factor: 7.446
  7 in total

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