Literature DB >> 18304814

Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.

Fabrizio Micheli1, Barbara Bertani, Andrea Bozzoli, Luca Crippa, Paolo Cavanni, Romano Di Fabio, Daniele Donati, Paola Marzorati, Giancarlo Merlo, Alfredo Paio, Lorenzo Perugini, Paola Zarantonello.   

Abstract

The synthesis and the structure activity of a new series of pyrrolo[1,2-a]pyrazine is reported. These molecules are potent and selective non-competitive mGluR5 antagonists and may shed new light on the pattern of substitution tolerated by this receptor.

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Year:  2008        PMID： 18304814     DOI： 10.1016/j.bmcl.2008.02.024

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


  6 in total

1.  Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.

Authors:  Santosh S Kulkarni; Mu-Fa Zou; Jianjing Cao; Jeffrey R Deschamps; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal:  J Med Chem       Date:  2009-06-11       Impact factor: 7.446

2.  Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.

Authors:  Ya Zhou; Alice L Rodriguez; Richard Williams; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-10-28       Impact factor: 2.823

3.  Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

Authors:  Alice L Rodriguez; Richard Williams; Ya Zhou; Stacey R Lindsley; Uyen Le; Mark D Grier; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-05-03       Impact factor: 2.823

4.  3-Methyl-1H-pyrrolo[2,1-c][1,4]oxazin-1-one.

Authors:  Salman Tariq Khan; Peng Yu; Erbin Hua; Syed Nawazish Ali; Mehrun Nisa
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-02-27

5.  3-Phenyl-1H-pyrrolo[2,1-c][1,4]oxazin-1-one.

Authors:  Salman Tariq Khan; Peng Yu; Suchada Chantrapromma; Yong-En Guo; Nighat Afza
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-05-26

6.  N-[2-(3-Methyl-1-oxo-1,2-dihydro-pyrrolo-[1,2-a]pyrazin-2-yl)eth-yl]methane-sulfonamide.

Authors:  Salman Tariq Khan; Peng Yu; Suchada Chantrapromma; Nighat Afza; Aisha Nelofar
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-07-10
  6 in total

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