Literature DB >> 17189691

Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.

Simona M Ceccarelli1, Georg Jaeschke, Bernd Buettelmann, Jörg Huwyler, Sabine Kolczewski, Jens-Uwe Peters, Eric Prinssen, Richard Porter, Will Spooren, Eric Vieira.   

Abstract

A novel class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the structure of the known anxiolytic fenobam. Representative compounds from this class show favorable pharmacokinetic properties and are active in an in vivo model of anxiety.

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Year:  2006        PMID: 17189691     DOI: 10.1016/j.bmcl.2006.12.006

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


  4 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

Review 2.  Allosteric modulation of metabotropic glutamate receptors.

Authors:  Douglas J Sheffler; Karen J Gregory; Jerri M Rook; P Jeffrey Conn
Journal:  Adv Pharmacol       Date:  2011

3.  Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().

Authors:  Moses G Gichinga; Jeremy P Olson; Elizabeth Butala; Hernán A Navarro; Brian P Gilmour; S Wayne Mascarella; F Ivy Carroll
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

4.  Synthesis of 1-isopropyl-3-acyl-5-methyl-benzimidazolone derivatives and their antimicrobial activity.

Authors:  Nan Xu; Chunnan Yang; Xinqi Gan; Shaopeng Wei; Zhiqin Ji
Journal:  Int J Mol Sci       Date:  2013-03-26       Impact factor: 5.923

  4 in total

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