Abstract
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
MeSH terms
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Amides / chemistry*
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Benzoxazines / chemistry
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Benzoxazines / pharmacology*
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Capsaicin / chemistry
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Carrier Proteins / antagonists & inhibitors
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Chemistry, Pharmaceutical / methods
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Drug Design
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Conformation
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Piperidines / chemistry*
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Protein Binding
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Quantitative Structure-Activity Relationship
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Structure-Activity Relationship
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TRPV Cation Channels / antagonists & inhibitors*
Substances
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Amides
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Benzoxazines
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Carrier Proteins
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Piperidines
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TRPV Cation Channels
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TRPV1 protein, human
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Capsaicin