Abstract
A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization.
Keywords:
Antagonist; Ligand gated ion channel; TRPA1.
Copyright © 2014 Elsevier Ltd. All rights reserved.
MeSH terms
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Calcium Channels
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Dose-Response Relationship, Drug
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Drug Discovery*
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Humans
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Isoquinolines / chemical synthesis
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Isoquinolines / chemistry
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Isoquinolines / pharmacology*
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Molecular Structure
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Nerve Tissue Proteins / antagonists & inhibitors*
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Pyridines / chemical synthesis
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Pyridines / chemistry
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Pyridines / pharmacology*
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Pyrroles / chemical synthesis
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Structure-Activity Relationship
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TRPA1 Cation Channel
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Transient Receptor Potential Channels / antagonists & inhibitors*
Substances
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Calcium Channels
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Isoquinolines
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Nerve Tissue Proteins
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Pyridines
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Pyrroles
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TRPA1 Cation Channel
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TRPA1 protein, human
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Transient Receptor Potential Channels