Literature DB >> 12798316

2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships.

Fabrizio Micheli1, Romano Di Fabio, Fabio Bordi, Palmina Cavallini, Paolo Cavanni, Daniele Donati, Stefania Faedo, Micaela Maffeis, Fabio Maria Sabbatini, Giorgio Tarzia, Maria Elvira Tranquillini.   

Abstract

Following the disclosure of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester [3,5-dimethyl PPP] as a potent and selective mGluR1 non-competitive antagonist, we report here further in vivo characterization of this important tool and disclose the investigation of the C-5 position, which led to very potent compounds.

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Year:  2003        PMID: 12798316     DOI: 10.1016/s0960-894x(03)00396-2

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


  2 in total

Review 1.  Molecular Basis for Modulation of Metabotropic Glutamate Receptors and Their Drug Actions by Extracellular Ca2.

Authors:  Juan Zou; Jason Y Jiang; Jenny J Yang
Journal:  Int J Mol Sci       Date:  2017-03-21       Impact factor: 5.923

2.  Synthesis and evaluation of novel pyrroles and pyrrolopyrimidines as anti-hyperglycemic agents.

Authors:  M S Mohamed; S A Ali; D H A Abdelaziz; Samar S Fathallah
Journal:  Biomed Res Int       Date:  2014-06-26       Impact factor: 3.411

  2 in total

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