Abstract
A series of N-propyl-8-chloro-6-substituted isoquinolones was identified as positive allosteric modulators of metabotropic glutamate receptor 2 (mGluR2 PAM) via high throughput screening (HTS). The subsequent synthesis and initial SAR exploration that led to the identification of compound 28 is described.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Allosteric Regulation
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High-Throughput Screening Assays
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Humans
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Microsomes, Liver / metabolism
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Quinolones / chemical synthesis
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Quinolones / chemistry*
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Quinolones / pharmacology
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Receptors, Metabotropic Glutamate / chemistry*
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Receptors, Metabotropic Glutamate / metabolism
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Structure-Activity Relationship
Substances
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Pyridines
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Quinolones
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2