Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.

PubWeight™: 1.00‹?› | Rank: Top 15%

🔗 View Article (PMID 15341479)

Published in J Med Chem on September 09, 2004

Authors

Jeffrey Roppe, Nicholas D Smith, Dehua Huang, Lida Tehrani, Bowei Wang, Jeffrey Anderson, Jesse Brodkin, Janice Chung, Xiaohui Jiang, Christopher King, Benito Munoz, Mark A Varney, Petpiboon Prasit, Nicholas D P Cosford

Articles citing this

Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett (2007) 1.54

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. Mol Pharmacol (2012) 1.15

Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett (2007) 1.04

Rapid multistep synthesis of 1,2,4-oxadiazoles in a single continuous microreactor sequence. J Org Chem (2008) 0.89

Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site. ACS Chem Neurosci (2014) 0.86

Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors. Bioorg Med Chem Lett (2013) 0.84

Investigation on tolerance development to subchronic blockade of mGluR5 in models of learning, anxiety, and levodopa-induced dyskinesia in rats. J Neural Transm (Vienna) (2008) 0.80

Metabotropic glutamate receptors: potential drug targets for psychiatric disorders. Open Med Chem J (2010) 0.79

Bis-aryloxadiazoles as effective activators of the aryl hydrocarbon receptor. Bioorg Med Chem Lett (2014) 0.76

Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. ACS Chem Biol (2016) 0.76

Continuous-flow synthesis of highly functionalized imidazo-oxadiazoles facilitated by microfluidic extraction. Beilstein J Org Chem (2017) 0.75

Articles by these authors

Mutant presenilins specifically elevate the levels of the 42 residue beta-amyloid peptide in vivo: evidence for augmentation of a 42-specific gamma secretase. Hum Mol Genet (2003) 5.92

ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res (2012) 2.51

Pakistan's reform experiment. Nature (2009) 2.35

An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules. Cell (2013) 2.30

Challenges in infant immunity: implications for responses to infection and vaccines. Nat Immunol (2011) 2.17

3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J Med Chem (2003) 2.17

Childhood cancer incidence in Pennsylvania counties in relation to living in counties with hydraulic fracturing sites. J Occup Environ Med (2013) 2.13

Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers. Synapse (2005) 1.90

Small molecules can selectively inhibit ephrin binding to the EphA4 and EphA2 receptors. J Biol Chem (2008) 1.80

Simulation of Ca2+ and Mg2+ solvation using polarizable atomic multipole potential. J Phys Chem B (2006) 1.73

Operative versus nonoperative treatment for acute Achilles tendon rupture: a meta-analysis based on current evidence. Int Orthop (2011) 1.73

DOVIS: an implementation for high-throughput virtual screening using AutoDock. BMC Bioinformatics (2008) 1.70

Towards patient-based cancer therapeutics. Nat Biotechnol (2010) 1.63

Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model. J Biol Chem (2010) 1.46

HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus. Assay Drug Dev Technol (2007) 1.40

Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J Pharmacol Exp Ther (2009) 1.40

Hypothermia: an unusual indication for gastric lavage. J Emerg Med (2009) 1.39

Electrocardiographic interpretation in athletes: the 'Seattle criteria'. Br J Sports Med (2013) 1.34

Chemical biology investigation of cell death pathways activated by endoplasmic reticulum stress reveals cytoprotective modulators of ASK1. J Biol Chem (2008) 1.33

In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). Eur J Pharmacol (2003) 1.33

Differential distribution of voltage-gated calcium channel alpha-2 delta (alpha2delta) subunit mRNA-containing cells in the rat central nervous system and the dorsal root ganglia. J Comp Neurol (2005) 1.27

Exploring eye movements in patients with glaucoma when viewing a driving scene. PLoS One (2010) 1.26

Correlation of Gleason scores with diffusion-weighted imaging findings of prostate cancer. Adv Urol (2011) 1.25

Tumor immunotherapy across MHC barriers using allogeneic T-cell precursors. Nat Biotechnol (2008) 1.24

The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats. Neuropsychopharmacology (2010) 1.23

The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety. Neuropsychopharmacology (2004) 1.23

Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol Pharmacol (2003) 1.23

STAT-3 and ERK 1/2 phosphorylation are critical for T-cell alloactivation and graft-versus-host disease. Blood (2008) 1.21

Preclinical studies of celastrol and acetyl isogambogic acid in melanoma. Clin Cancer Res (2007) 1.20

Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897. Biochem Pharmacol (2005) 1.20

[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett (2003) 1.19

Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system. Anal Biochem (2003) 1.19

Phosphomannose isomerase inhibitors improve N-glycosylation in selected phosphomannomutase-deficient fibroblasts. J Biol Chem (2011) 1.19

Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). J Med Chem (2009) 1.13

Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J Pharmacol Exp Ther (2004) 1.13

A survey of state medical licensing boards: can the travelling team physician practice in your state? Br J Sports Med (2012) 1.13

A randomized, double-blind, placebo-controlled assessment of BMS-936558, a fully human monoclonal antibody to programmed death-1 (PD-1), in patients with chronic hepatitis C virus infection. PLoS One (2013) 1.12

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria. ACS Med Chem Lett (2011) 1.12

Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Bioorg Med Chem Lett (2008) 1.11

5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. Bioorg Med Chem Lett (2004) 1.10

Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg Med Chem Lett (2011) 1.10

Factors affecting growth in infants with single ventricle physiology: a report from the Pediatric Heart Network Infant Single Ventricle Trial. J Pediatr (2011) 1.09

Characterization of mouse orofacial pain and the effects of lesioning TRPV1-expressing neurons on operant behavior. Mol Pain (2008) 1.08

Anxiolytic-like activity of the mGluR5 antagonist MPEP: a comparison with diazepam and buspirone. Pharmacol Biochem Behav (2002) 1.08

A Prospective Study of Overuse Knee Injuries Among Female Athletes With Muscle Imbalances and Structural Abnormalities. J Athl Train (2004) 1.07

Self-report of alcohol use for pain in a multi-ethnic community sample. J Pain (2009) 1.07

Loss of seven-up from Drosophila R1/R6 photoreceptors reveals a stochastic fate choice that is normally biased by Notch. Development (2008) 1.04

Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton. J Pharmacol Exp Ther (2007) 1.04

Outcomes of endolymphatic shunt surgery for Ménière's disease: comparison with intratympanic gentamicin on vertigo control and hearing loss. Otol Neurotol (2010) 1.04

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorg Med Chem Lett (2012) 1.03

Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. Bioorg Med Chem Lett (2013) 1.03

Investigation of potential mechanisms regulating protein expression of hepatic pyruvate dehydrogenase kinase isoforms 2 and 4 by fatty acids and thyroid hormone. Biochem J (2003) 1.03

Reaction kinetics of degradation and epimerization of epigallocatechin gallate (EGCG) in aqueous system over a wide temperature range. J Agric Food Chem (2008) 1.02

[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther (2002) 1.02

How does glaucoma look?: patient perception of visual field loss. Ophthalmology (2013) 1.02

Evaluation of the role of peroxisome-proliferator-activated receptor alpha in the regulation of cardiac pyruvate dehydrogenase kinase 4 protein expression in response to starvation, high-fat feeding and hyperthyroidism. Biochem J (2002) 1.01

A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptors. Chem Biol Drug Des (2011) 1.01

CAPRISA 004 tenofovir microbicide trial: no impact of tenofovir gel on the HIV transmission bottleneck. J Infect Dis (2012) 0.99

In silico analyses of substrate interactions with human serum paraoxonase 1. Proteins (2009) 0.99

Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology (2004) 0.99

Spectroscopic studies on the interaction between tetrandrine and two serum albumins by chemometrics methods. Spectrochim Acta A Mol Biomol Spectrosc (2013) 0.99

Normal electrocardiographic findings: recognising physiological adaptations in athletes. Br J Sports Med (2013) 0.99

Fully automated continuous flow synthesis of highly functionalized imidazo[1,2-a] heterocycles. Org Lett (2010) 0.98

DEPBT as an efficient coupling reagent for amide bond formation with remarkable resistance to racemization. Biopolymers (2005) 0.97

Glaucoma and reading: exploring the effects of contrast lowering of text. Optom Vis Sci (2012) 0.97

Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators. ACS Chem Neurosci (2011) 0.97

Identification of a selective small molecule inhibitor of breast cancer stem cells. Bioorg Med Chem Lett (2012) 0.97

KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling. Mol Cancer Ther (2008) 0.95

Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists. J Med Chem (2006) 0.95

Total synthesis of ionomycin using ring-opening strategies. Org Lett (2002) 0.95

Life stories and biography: a means of connecting family and staff to people with dementia. J Clin Nurs (2010) 0.94

Image-guided radiotherapy in near real time with intensity-modulated radiotherapy megavoltage treatment beam imaging. Int J Radiat Oncol Biol Phys (2009) 0.94

Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNOS dimerization inhibitors that are orally active in pain models. J Med Chem (2010) 0.93

Structural, kinetic, and pharmacodynamic mechanisms of D-amino acid oxidase inhibition by small molecules. J Med Chem (2013) 0.93