Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.

No abstract is available for this paper.

• Publication year

  2018

• Venue

  European journal of medicinal chemistry

• Publication date

  2018-01-20

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.ejmech.2017.12.054PMID 29289890
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity.

  2017cited by this paper
• Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors.

  2017cited by this paper
• Design, Synthesis, Pharmacological Evaluation and Docking Studies of GluN2B‐Selective NMDA Receptor Antagonists with a Benzo[7]annulen‐7‐amine Scaffold

  2017cited by this paper
• Mechanism of NMDA Receptor Inhibition and Activation.

  2016cited by this paper
• A Novel Binding Mode Reveals Two Distinct Classes of NMDA Receptor GluN2B-selective Antagonists

  2016cited by this paper
• Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN).

  2016cited by this paper
• Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.

  2016cited by this paper
• Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.

  2015cited by this paper
• Enantiomerically Pure 2-Methyltetrahydro-3-benzazepin-1-ols Selectively Blocking GluN2B Subunit Containing N-Methyl-D-aspartate Receptors.

  2015cited by this paper
• Clay-Supported Cu(II) Catalyst: An Efficient, Heterogeneous, and Recyclable Catalyst for Synthesis of 1,4-Disubstituted 1,2,3-Triazoles from Alloxan-Derived Terminal Alkyne and Substituted Azides Using Click Chemistry

  2015cited by this paper
• GluN2B‐Selective N‐Methyl‐d‐aspartate (NMDA) Receptor Antagonists Derived from 3‐Benzazepines: Synthesis and Pharmacological Evaluation of Benzo[7]annulen‐7‐amines

  2014cited by this paper
• Metabolism studies of ifenprodil, a potent GluN2B receptor antagonist.

  2014cited by this paper
• Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.

  2014cited by this paper
• Synthesis and pharmacological evaluation of like- and unlike-configured tetrahydro-2-benzazepines with the α-substituted benzyl moiety in the 5-position.

  2014cited by this paper
• Synthesis and σ receptor affinity of regioisomeric spirocyclic furopyridines.

  2014cited by this paper
• In vitro and in vivo biotransformation of WMS-1410, a potent GluN2B selective NMDA receptor antagonist.

  2014cited by this paper
• Reduction of 2,2,2-trichloro-1-arylethanones by RMgX: mechanistic investigation and the synthesis of substituted α,α-dichloroketones.

  2013cited by this paper
• Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.

  2013cited by this paper
• NMDA receptors in nervous system diseases.

  2013cited by this paper
• NMDA Receptor Activity in Neuropsychiatric Disorders

  2013cited by this paper
• NMDA receptor subunit diversity: impact on receptor properties, synaptic plasticity and disease

  2013cited by this paper
• Synapses and Alzheimer's disease.

  2012cited by this paper
• Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.

  2012cited by this paper
• Neuropsin cleaves EphB2 in the amygdala to control anxiety

  2011cited by this paper
• Soluble Aβ Oligomers Inhibit Long-Term Potentiation through a Mechanism Involving Excessive Activation of Extrasynaptic NR2B-Containing NMDA Receptors

  2011cited by this paper
• Early neuronal dysfunction by amyloid β oligomers depends on activation of NR2B-containing NMDA receptors.

  2011cited by this paper
• Design, Synthesis, and Biological Evaluation of 3‐Benzazepin‐1‐ols as NR2B‐Selective NMDA Receptor Antagonists

  2010cited by this paper
• Synthesis and SAR studies of chiral non-racemic dexoxadrol analogues as uncompetitive NMDA receptor antagonists.

  2010cited by this paper
• Organikum1: Organisch‐chemisches Grundpraktikum

  2010cited by this paper
• Development of a selective competitive receptor binding assay for the determination of the affinity to NR2B containing NMDA receptors.

  2010cited by this paper
• GluN2B subunit-containing NMDA receptor antagonists prevent Aβ-mediated synaptic plasticity disruption in vivo

  2009cited by this paper
• Structure–Activity Relationship in the Domain of Odorants Having Marine Notes

  2007cited by this paper
• Human sulfotransferases and their role in chemical metabolism.

  2006cited by this paper
• Synthesis of Aromatic Aldehydes by Oxidative Hydroxymethylation

  2004cited by this paper
• Huntington's disease

  2001cited by this paper
• Human UDP-glucuronosyltransferases: metabolism, expression, and disease.

  2000cited by this paper
• Ibogaine possesses a selective affinity for sigma 2 receptors.

  1995cited by this paper
• Ibogaine possesses a selective affinity for σ2 receptors

  1995cited by this paper
• Characterization of the binding of [3H](+)-pentazocine to σ recognition sites in guinea pig brain

  1992cited by this paper
• Characterization of the binding of [3H](+)-pentazocine to sigma recognition sites in guinea pig brain.

  1992cited by this paper
• Experimental Organic Chemistry

  1989cited by this paper
• Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

  1973cited by this paper
• 142. Organic fluoro-compounds. Part IV. The hoesch reaction with trifluoromethyl and trichloromethyl cyanides

  1951cited by this paper
• The Catalytic Dehydrogenation of 2-Substituted-5,6,7,8-tetrahydronaphthalene Derivatives1

  1943cited by this paper

• Phenol (bio)isosteres in drug design and development

  2024cites this paper
• Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.

  2023cites this paper
• An in-silico investigation based on molecular simulations of novel and potential brain-penetrant GluN2B NMDA receptor antagonists as anti-stroke therapeutic agents

  2023cites this paper
• GluN2B subunit selective N-methyl-D-aspartate receptor ligands: Democratizing recent progress to assist the development of novel neurotherapeutics

  2023cites this paper
• Drug/Lead Compound Hydroxymethylation as a Simple Approach to Enhance Pharmacodynamic and Pharmacokinetic Properties

  2022cites this paper
• Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.

  2022cites this paper
• GluN2B/N-methyl-D-aspartate receptor antagonists: Advances in design, synthesis, and pharmacological evaluation studies.

  2021cites this paper
• Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.

  2021cites this paper
• [2.2]Paracyclophane‐Based TCN‐201 Analogs as GluN2A‐Selective NMDA Receptor Antagonists

  2021cites this paper
• A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists.

  2020cites this paper
• Synthesis of GluN2A-selective NMDA receptor antagonists with an electron-rich aromatic B-ring.

  2020cites this paper
• Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.

  2019cites this paper
• Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation.

  2019cites this paper
• Comprehensive QSAR studies reveal structural insights into the NR2B subtype selective benzazepine derivatives as N-Methyl- -Aspartate receptor antagonists

  2019cites this paper
• Replacement of the Benzylpiperidine Moiety with Fluorinated Phenylalkyl Side Chains for the Development of GluN2B Receptor Ligands

  2018cites this paper
• Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents.

  2018cites this paper