Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.

No abstract is available for this paper.

• Publication year

  2010

• Venue

  Bioorganic & Medicinal Chemistry Letters

• Publication date

  2010-06-15

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.bmcl.2010.04.075PMID 20483612
• 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.

• Simple Size-Independent Measure of Ligand Efficiency

  2009cited by this paper
• The influence of lead discovery strategies on the properties of drug candidates

  2009cited by this paper
• mGlu5 receptor antagonists and their therapeutic potential

  2008cited by this paper
• Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity

  2005cited by this paper
• NR2B subunit selective NMDA antagonists inhibit neurotoxic effect of alcohol-withdrawal in primary cultures of rat cortical neurones.

  2004cited by this paper
• A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain

  2004cited by this paper
• [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.

  2002cited by this paper
• Parallel synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation

  2001cited by this paper
• Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice

  2001cited by this paper
• Potential anxiolytic‐ and antidepressant‐like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist

  2001cited by this paper
• mGluR5 antagonists 2-methyl-6-(phenylethynyl)-pyridine and (E)-2-methyl-6-(2-phenylethenyl)-pyridine reduce traumatic neuronal injury in vitro and in vivo by antagonizing N-methyl-D-aspartate receptors.

  2001cited by this paper
• Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders.

  2001cited by this paper
• Blockade of the metabotropic glutamate receptor subtype 5 (mGluR5) produces antiparkinsonian-like effects in rats.

  2001cited by this paper
• Coordinate regulation of metabotropic glutamate receptors.

  2001cited by this paper
• Synthesis of 3,5-disubstituted-1,2,4-oxadiazoles using tetrabutylammonium fluoride as a mild and efficient catalyst

  2001cited by this paper
• mGlu5 receptors and nociceptive function II. mGlu5 receptors functionally expressed on peripheral sensory neurones mediate inflammatory hyperalgesia.

  2001cited by this paper
• Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893).

  2000cited by this paper
• Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents.

  2000cited by this paper
• Selective blockade of metabotropic glutamate receptor subtype 5 is neuroprotective.

  2000cited by this paper
• Synthesis and activity of 3-pyridylamine ligands at central nicotinic receptors.

  2000cited by this paper
• New entry to alicyclic amines via alkylative fragmentation of cyclic aminoaldehyde tosylhydrazones

  2000cited by this paper
• Group I metabotropic glutamate receptors: implications for brain diseases.

  1999cited by this paper
• Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain

  1995cited by this paper
• The metabotropic glutamate receptors: structure and functions.

  1995cited by this paper
• Novel functions for subtypes of metabotropic glutamate receptors.

  1994cited by this paper
• Metabotropic glutamate receptors in brain function and pathology.

  1993cited by this paper
• Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study.

  1982cited by this paper
• AZO COUPLING OF BENZENESULFONYLHYDRAZONES OF HETEROCYCLIC ALDEHYDES

  1979cited by this paper
• A facile synthesis of 2,5-disubstituted tetrazoles by the reaction of phenylsulfonylhydrazones with arenediazonium salts.

  1976cited by this paper

• Room Temperature Synthesis of Bioactive 1,2,4-Oxadiazoles

  2023cites this paper
• Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5

  2022cites this paper
• The reaction of amidoximes with carboxylic acids or their esters under high-pressure conditions

  2019cites this paper
• 4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.

  2016cites this paper
• Comparative functional studies on cell lines expressing recombinant receptors

  2016cites this paper
• Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators.

  2015cites this paper
• Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization.

  2015cites this paper
• Small Molecule Therapeutics for Schizophrenia

  2015cites this paper
• Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization.

  2014cites this paper
• Activation of the mGlu5 Receptor for the Treatment of Schizophrenia and Cognitive-Deficit-Associated Disorders

  2014cites this paper
• Substituted oxadiazoles: a patent review (2010 – 2012)

  2013cites this paper
• Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).

  2013cites this paper
• Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.

  2013cites this paper
• Stereoselective approach to cis-2,3-disubstituted piperidines via reduction of N-acyliminium ion intermediate: enantioselective synthesis of (+)-(2S,3S)-CP-99,994.

  2012cites this paper
• Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

  2012cites this paper
• mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders

  2012cites this paper
• Recent advances in the design and development of novel negative allosteric modulators of mGlu(5).

  2011cites this paper
• 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.

  2011cites this paper
• Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

  2011cites this paper
• Fragile X syndrome: an update on developing treatment modalities.

  2011cites this paper
• Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.

  2011cites this paper
• Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.

  2010cites this paper