ArticleJournal of medicinal chemistry2015
Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Discovery of VU6066098: A Selective and CNS-Penetrant mGluACS chemical neuroscience · 2026Article
- Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.ACS medicinal chemistry letters · 2023Article
- The role of thalamic group II mGlu receptors in health and disease.Neuronal signaling · 2022Review
- Synthesis and Characterization of 5-(2-Fluoro-4-[Journal of medicinal chemistry · 2022Article
- Targeting metabotropic glutamate receptors for the treatment of depression and other stress-related disorders.Neuropharmacology · 2021Review
- Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[Journal of medicinal chemistry · 2020Article
- Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logACS medicinal chemistry letters · 2019Article
- Palladium-Catalysed Synthesis and Transformation of Quinolones.Molecules (Basel, Switzerland) · 2019Review
- Study on the regioselectivity of the N-ethylation reaction ofBeilstein journal of organic chemistry · 2019Article
- Differential Pharmacology and Binding of mGluMolecular pharmacology · 2018Article
- Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[ACS chemical neuroscience · 2017Article
- Design and Synthesis of mGluACS medicinal chemistry letters · 2017Article
- Design and Synthesis ofACS medicinal chemistry letters · 2017Article
- Metabotropic glutamate receptor 2 inhibits thalamically-driven glutamate and dopamine release in the dorsal striatum.Neuropharmacology · 2017Article
- Recent advances in the medicinal chemistry of group II and group III mGlu receptors.MedChemComm · 2017Review
- Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.Chemical reviews · 2016Review
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15 authors.
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Abstract
Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu2/3 inhibition and a variety of CNS diseases and disorders. Though these tools typically have good selectivity for mGlu2/3 versus the remaining six members of the mGlu family, compounds that are selective for only one of the individual group II mGlus have proved elusive. Herein we report on the discovery of a potent and highly selective mGlu2 negative allosteric modulator 58 (VU6001192) from a series of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides. The concept for the design of this series centered on morphing a quinoline series recently disclosed in the patent literature into a chemotype previously used for the preparation of muscarinic acetylcholine receptor subtype 1 positive allosteric modulators. Compound 58 exhibits a favorable profile and will be a useful tool for understanding the biological implications of selective inhibition of mGlu2 in the CNS.
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