Literature DB >> 16678408

Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.

Santosh S Kulkarni1, Barbara Nightingale, Christina M Dersch, Richard B Rothman, Amy Hauck Newman.   

Abstract

A series of diaryl amides was designed and synthesized as novel nonethynyl mGluR5 antagonists. The systematic variation of the pharmacophoric groups led to the identification of a lead compound that demonstrated micromolar affinity for the mGluR5. Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro.

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Year:  2006        PMID： 16678408     DOI： 10.1016/j.bmcl.2006.04.032

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


  9 in total

1.  Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.

Authors:  Santosh S Kulkarni; Amy Hauck Newman
Journal:  Bioorg Med Chem Lett       Date:  2007-01-04       Impact factor: 2.823

2.  Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.

Authors:  Santosh S Kulkarni; Amy Hauck Newman
Journal:  Bioorg Med Chem Lett       Date:  2007-03-24       Impact factor: 2.823

3.  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

4.  Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.

Authors:  Peng Zhang; Mu-Fa Zou; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal:  Bioorg Med Chem       Date:  2010-03-27       Impact factor: 3.641

5.  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

6.  Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.

Authors:  Mu-Fa Zou; Jianjing Cao; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal:  Bioorg Med Chem Lett       Date:  2010-12-28       Impact factor: 2.823

7.  Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.

Authors:  Thomas M Keck; Mu-Fa Zou; Peng Zhang; Rebecca P Rutledge; Amy Hauck Newman
Journal:  ACS Med Chem Lett       Date:  2012-05-22       Impact factor: 4.345

8.  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

9.  Chemodivergent synthesis of N-(pyridin-2-yl)amides and 3-bromoimidazo[1,2-a]pyridines from α-bromoketones and 2-aminopyridines.

Authors:  Yanpeng Liu; Lixue Lu; Haipin Zhou; Feijie Xu; Cong Ma; Zhangjian Huang; Jinyi Xu; Shengtao Xu
Journal:  RSC Adv       Date:  2019-10-28       Impact factor: 4.036
  9 in total

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