Literature DB >> 20346665

A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.

T K Sasikumar1, Li Qiang, Duane A Burnett, William J Greenlee, Cheng Li, Mariagrazia Grilli, Rosalia Bertorelli, Gianluca Lozza, Angelo Reggiani.   

Abstract

A-ring modifications on the triazafluorenone core structure were investigated. Five membered heterocycles such as pyrazoles and isothiazoles are not tolerated. It has been found that the pyrimidine nucleus was very well tolerated on the left hand side. Amino pyrimidine compounds 24 and 27 showed acceptable PK profile with significant brain penetration. Compound 9 served as a versatile intermediate for a number of chemical transformations. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20346665     DOI： 10.1016/j.bmcl.2010.03.004

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


  6 in total

Review 1.  Recent advances in the medicinal chemistry of the metabotropic glutamate receptor 1 (mGlu₁).

Authors:  Dafydd R Owen
Journal:  ACS Chem Neurosci       Date:  2011-03-10       Impact factor: 4.418

2.  A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.

Authors:  Hyekyung P Cho; Darren W Engers; Daryl F Venable; Colleen M Niswender; Craig W Lindsley; P Jeffrey Conn; Kyle A Emmitte; Alice L Rodriguez
Journal:  ACS Chem Neurosci       Date:  2014-05-15       Impact factor: 4.418

3.  Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

Authors:  Kasper Harpsøe; Vignir Isberg; Benjamin G Tehan; Dahlia Weiss; Angela Arsova; Fiona H Marshall; Hans Bräuner-Osborne; David E Gloriam
Journal:  Sci Rep       Date:  2015-09-11       Impact factor: 4.379

4.  Chronic pain and adult hippocampal neurogenesis: translational implications from preclinical studies.

Authors:  Mariagrazia Grilli
Journal:  J Pain Res       Date:  2017-09-21       Impact factor: 3.133

Review 5.  Opiate Analgesics as Negative Modulators of Adult Hippocampal Neurogenesis: Potential Implications in Clinical Practice.

Authors:  Valeria Bortolotto; Mariagrazia Grilli
Journal:  Front Pharmacol       Date:  2017-05-09       Impact factor: 5.810

6.  Chronic Treatment with Fluoxetine Induces Sex-Dependent Analgesic Effects and Modulates HDAC2 and mGlu2 Expression in Female Mice.

Authors:  Magda Zammataro; Sara Merlo; Massimo Barresi; Carmela Parenti; Huijuan Hu; Maria A Sortino; Santina Chiechio
Journal:  Front Pharmacol       Date:  2017-10-20       Impact factor: 5.810
  6 in total

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