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Literature DB >> 29125762

Highly Selective Dopamine D₃ Receptor Antagonists with Arylated Diazaspiro Alkane Cores.

Sean W Reilly¹, Suzy Griffin², Michelle Taylor², Kristoffer Sahlholm¹, Chi-Chang Weng¹, Kuiying Xu¹, Daniel A Jacome³, Robert R Luedtke², Robert H Mach¹.

Abstract

A series of potent and selective D3 receptor (D3R) analogues with diazaspiro alkane cores were synthesized. Radioligand binding of compounds 11, 14, 15a, and 15c revealed favorable D3R affinity (Ki = 12-25.6 nM) and were highly selective for D3R vs D3R (ranging from 264- to 905-fold). Variation of these novel ligand architectures can be achieved using our previously reported 10-20 min benchtop C-N cross-coupling methodology, affording a broad range of arylated diazaspiro precursors.

Entities: CellLine Chemical Disease Gene Species

Mesh：

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Year: 2017 PMID： 29125762 PMCID： PMC5767125 DOI： 10.1021/acs.jmedchem.7b01248

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

34 in total

Review 1. Progress in developing D3 dopamine receptor ligands as potential therapeutic agents for neurological and neuropsychiatric disorders.

Authors: Robert R Luedtkea; Robert H Mach
Journal: Curr Pharm Des Date: 2003 Impact factor: 3.116

2. Distribution of dopamine D3 receptor expressing neurons in the human forebrain: comparison with D2 receptor expressing neurons.

Authors: E V Gurevich; J N Joyce
Journal: Neuropsychopharmacology Date: 1999-01 Impact factor: 7.853

Review 3. Recent advances in the development of dopamine D3 receptor antagonists: a medicinal chemistry perspective.

Authors: Fabrizio Micheli
Journal: ChemMedChem Date: 2011-03-18 Impact factor: 3.466

Review 4. Novel, Selective, and Developable Dopamine D₃ Antagonists with a Modified "Amino" Region.

Authors: Fabrizio Micheli
Journal: ChemMedChem Date: 2017-05-05 Impact factor: 3.466

Review 5. Current drug treatments targeting dopamine D3 receptor.

Authors: Gian Marco Leggio; Claudio Bucolo; Chiara Bianca Maria Platania; Salvatore Salomone; Filippo Drago
Journal: Pharmacol Ther Date: 2016-06-22 Impact factor: 12.310

6. 1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.

Authors: Fabrizio Micheli; Alessia Bacchi; Simone Braggio; Laura Castelletti; Palmina Cavallini; Paolo Cavanni; Susanna Cremonesi; Michele Dal Cin; Aldo Feriani; Sylvie Gehanne; Mahmud Kajbaf; Luciano Marchió; Selena Nola; Beatrice Oliosi; Annalisa Pellacani; Elisabetta Perdonà; Anna Sava; Teresa Semeraro; Luca Tarsi; Silvia Tomelleri; Andrea Wong; Filippo Visentini; Laura Zonzini; Christian Heidbreder
Journal: J Med Chem Date: 2016-09-09 Impact factor: 7.446

Review 7. Targeting the dopamine D3 receptor: an overview of drug design strategies.

Authors: Antoni Cortés; Estefanía Moreno; Mar Rodríguez-Ruiz; Enric I Canela; Vicent Casadó
Journal: Expert Opin Drug Discov Date: 2016-05-30 Impact factor: 6.098

8. Occupancy of brain dopamine D3 receptors and drug craving: a translational approach.

Authors: Manolo Mugnaini; Laura Iavarone; Palmina Cavallini; Cristiana Griffante; Beatrice Oliosi; Chiara Savoia; John Beaver; Eugenii A Rabiner; Fabrizio Micheli; Christian Heidbreder; Anne Andorn; Emilio Merlo Pich; Massimo Bani
Journal: Neuropsychopharmacology Date: 2012-09-12 Impact factor: 7.853

9. 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.

Authors: Fabrizio Micheli; Luca Arista; Giorgio Bonanomi; Frank E Blaney; Simone Braggio; Anna Maria Capelli; Anna Checchia; Federica Damiani; Romano Di-Fabio; Stefano Fontana; Gabriella Gentile; Cristiana Griffante; Dieter Hamprecht; Carla Marchioro; Manolo Mugnaini; Jacqui Piner; Emiliangelo Ratti; Giovanna Tedesco; Luca Tarsi; Silvia Terreni; Angela Worby; Charles R Ashby; Christian Heidbreder
Journal: J Med Chem Date: 2010-01-14 Impact factor: 7.446

10. 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.

Authors: Fabrizio Micheli; Giorgio Bonanomi; Frank E Blaney; Simone Braggio; Anna Maria Capelli; Anna Checchia; Ornella Curcuruto; Federica Damiani; Romano Di Fabio; Daniele Donati; Gabriella Gentile; Andy Gribble; Dieter Hamprecht; Giovanna Tedesco; Silvia Terreni; Luca Tarsi; Andrew Lightfoot; Geoff Stemp; Gregor Macdonald; Alex Smith; Michela Pecoraro; Marcella Petrone; Ornella Perini; Jacqui Piner; Tino Rossi; Angela Worby; Maria Pilla; Enzo Valerio; Cristiana Griffante; Manolo Mugnaini; Martyn Wood; Claire Scott; Michela Andreoli; Laurent Lacroix; Adam Schwarz; Alessandro Gozzi; Angelo Bifone; Charles R Ashby; Jim J Hagan; Christian Heidbreder
Journal: J Med Chem Date: 2007-09-15 Impact factor: 7.446

8 in total

1. Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.

Authors: Sean W Reilly; Laura N Puentes; Khadija Wilson; Chia-Ju Hsieh; Chi-Chang Weng; Mehran Makvandi; Robert H Mach
Journal: J Med Chem Date: 2018-06-14 Impact factor: 7.446

Highly Selective Dopamine D₃ Receptor Antagonists with Arylated Diazaspiro Alkane Cores.

Review 1. Progress in developing D3 dopamine receptor ligands as potential therapeutic agents for neurological and neuropsychiatric disorders.

2. Distribution of dopamine D3 receptor expressing neurons in the human forebrain: comparison with D2 receptor expressing neurons.

Review 3. Recent advances in the development of dopamine D3 receptor antagonists: a medicinal chemistry perspective.

Review 4. Novel, Selective, and Developable Dopamine D₃ Antagonists with a Modified "Amino" Region.

Review 5. Current drug treatments targeting dopamine D3 receptor.

6. 1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.

Review 7. Targeting the dopamine D3 receptor: an overview of drug design strategies.

8. Occupancy of brain dopamine D3 receptors and drug craving: a translational approach.

9. 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.

10. 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.

1. Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.

Review 2. Selectivity of probes for PET imaging of dopamine D3 receptors.

3. Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist.

Review 4. Principle and design of pseudo-natural products.

5. New Drugs, Old Targets: Tweaking the Dopamine System to Treat Psychostimulant Use Disorders.

Review 6. Neuronal Dopamine D3 Receptors: Translational Implications for Preclinical Research and CNS Disorders.

7. Identification of Novel Dopamine D₂ Receptor Ligands-A Combined In Silico/In Vitro Approach.

8. Exploration of Diazaspiro Cores as Piperazine Bioisosteres in the Development of σ2 Receptor Ligands.

Review 1. Progress in developing D3 dopamine receptor ligands as potential therapeutic agents for neurological and neuropsychiatric disorders.

Review 3. Recent advances in the development of dopamine D3 receptor antagonists: a medicinal chemistry perspective.

Review 4. Novel, Selective, and Developable Dopamine D3 Antagonists with a Modified "Amino" Region.

Review 5. Current drug treatments targeting dopamine D3 receptor.

Review 7. Targeting the dopamine D3 receptor: an overview of drug design strategies.

Review 2. Selectivity of probes for PET imaging of dopamine D3 receptors.

Review 4. Principle and design of pseudo-natural products.

Review 6. Neuronal Dopamine D3 Receptors: Translational Implications for Preclinical Research and CNS Disorders.

Review 4. Novel, Selective, and Developable Dopamine D₃ Antagonists with a Modified "Amino" Region.