Gabriella Gentile

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists
    Gabriella Gentile
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 17:5218-21. 2007
  2. ncbi 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists
    Fabrizio Micheli
    Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
    J Med Chem 53:374-91. 2010
  3. ncbi New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems
    Fabrizio Micheli
    GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 18:901-7. 2008
  4. ncbi New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems
    Fabrizio Micheli
    GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 18:908-12. 2008
  5. ncbi Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists
    Fabrizio Micheli
    Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
    J Med Chem 53:7129-39. 2010
  6. ncbi Heteroaryl-substituted 4-(1H-pyrazol-1-yl)-5,6-dihydro-1H-pyrrolo[2,3-d]pyrimidine derivatives as potent and selective corticotropin-releasing factor receptor-1 antagonists
    Fabio Maria Sabbatini
    Department of Medicinal Chemistry, Psychiatry Centre of Excellence for Drug Discovery (CEDD, Medicines Research Centre, GlaxoSmithKline SpA, Via A. Fleming 4, 37135 Verona, Italy
    ChemMedChem 3:226-9. 2008
  7. ncbi Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists
    Romano Di Fabio
    Neurosciences Centre of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy
    J Med Chem 51:7370-9. 2008
  8. ncbi Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization
    Fabrizio Micheli
    GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicine Research Centre, Verona, Italy
    Bioorg Med Chem Lett 19:4011-3. 2009
  9. ncbi 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors
    Gabriella Gentile
    Department of Medicinal Chemistry, Neuroscience Centre of Excellence of Drug Discovery, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 22:1989-94. 2012
  10. ncbi Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists
    Roberto Arban
    Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Verona, Italy
    Bioorg Med Chem Lett 20:5044-9. 2010

Detail Information

Publications17

  1. ncbi Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists
    Gabriella Gentile
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 17:5218-21. 2007
    ..Unsaturated tetrahydrotriazaacenaphthylenes of general structure 3 have been identified as potent and selective CRF(1) receptor antagonists with a suitable oral pharmacokinetic profile...
  2. ncbi 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists
    Fabrizio Micheli
    Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
    J Med Chem 53:374-91. 2010
    ..Several members of this series also significantly attenuate the expression of conditioned place preference (CPP) to nicotine and cocaine...
  3. ncbi New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems
    Fabrizio Micheli
    GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 18:901-7. 2008
    ..The introduction of a tricyclic [h]-fused benzazepine moiety on the recently disclosed scaffold of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines is reported. A full rat pharmacokinetic characterization is also reported...
  4. ncbi New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems
    Fabrizio Micheli
    GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 18:908-12. 2008
    ..The new scaffolds of the [g]-fused and the hetero-fused tricyclic benzazepine are here reported together with their pharmacokinetic profile...
  5. ncbi Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists
    Fabrizio Micheli
    Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
    J Med Chem 53:7129-39. 2010
    ..In this manuscript, we are reporting a detailed exploration of the region of the receptor interacting with the amine terminus of the scaffold wherein SAR and developability data associated with these novel templates was undertaken...
  6. ncbi Heteroaryl-substituted 4-(1H-pyrazol-1-yl)-5,6-dihydro-1H-pyrrolo[2,3-d]pyrimidine derivatives as potent and selective corticotropin-releasing factor receptor-1 antagonists
    Fabio Maria Sabbatini
    Department of Medicinal Chemistry, Psychiatry Centre of Excellence for Drug Discovery (CEDD, Medicines Research Centre, GlaxoSmithKline SpA, Via A. Fleming 4, 37135 Verona, Italy
    ChemMedChem 3:226-9. 2008
  7. ncbi Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists
    Romano Di Fabio
    Neurosciences Centre of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy
    J Med Chem 51:7370-9. 2008
    ....
  8. ncbi Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization
    Fabrizio Micheli
    GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicine Research Centre, Verona, Italy
    Bioorg Med Chem Lett 19:4011-3. 2009
    ..The lead optimization process to identify new selective dopamine D(3) receptor antagonists is reported. DMPK parameters and binding data suggest that selective D(3) receptor antagonists as potential PET ligands might have been identified...
  9. ncbi 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors
    Gabriella Gentile
    Department of Medicinal Chemistry, Neuroscience Centre of Excellence of Drug Discovery, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 22:1989-94. 2012
    ..5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors. The optimization of the series to yield compounds with cell activity and brain permeability is described...
  10. ncbi Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists
    Roberto Arban
    Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Verona, Italy
    Bioorg Med Chem Lett 20:5044-9. 2010
    ....
  11. ncbi [3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonists
    Fabrizio Micheli
    Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 20:5491-4. 2010
    ..A new class of azabicyclo[3.1.0]benzenesulfonamides is presented as selective dopamine D3 antagonists together with SAR and selectivity data...
  12. ncbi 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists
    Fabrizio Micheli
    Psychiatry Centre of Excellence, Molecular Discovery Research, and Safety Assessment, GlaxoSmithKline Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy
    J Med Chem 50:5076-89. 2007
    ....
  13. ncbi Identification of 2-(4-pyridyl)thienopyridinones as GSK-3? inhibitors
    Gabriella Gentile
    Department of Medicinal Chemistry, Neuroscience Centre of Excellence of Drug Discovery, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 21:4823-7. 2011
    ..X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented...
  14. ncbi In vivo quantification of regional dopamine-D3 receptor binding potential of (+)-PHNO: Studies in non-human primates and transgenic mice
    Eugenii A Rabiner
    GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, UK
    Synapse 63:782-93. 2009
    ..The midbrain is thus an excellent target region to examine D3 receptor occupancy with [(11)C]-(+)-PHNO PET in vivo...
  15. ncbi Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies
    Romano Di Fabio
    Neurosciences Centre of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135, Verona, Italy
    J Med Chem 51:7273-86. 2008
    ....
  16. ncbi Chiral tetrahydroquinoline derivatives as potent anti-hyperalgesic agents in animal models of sustained inflammation and chronic neuropathic pain
    Romano Di Fabio
    GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy
    Bioorg Med Chem Lett 17:1176-80. 2007
    ..This efficient route enabled to scale up the synthesis of an orally bioavailable glycine antagonist showing outstanding in vivo anti-hyperalgesic activity in different animal models of sustained inflammation and chronic neuropathic pain...
  17. ncbi Cyclopenta[d]pyrimidines and dihydropyrrolo[2,3-d]pyrimidines as potent and selective corticotropin-releasing factor 1 receptor antagonists
    Roberto Arban
    GlaxoSmithKline Medicines Center, Psychiatry CEDD, Via A Fleming 4, 37135 Verona, Italy
    ChemMedChem 2:528-40. 2007
    ....