Abstract
We report on a series of alpha-substituted-beta-tetralin-derived and related phenethyl-based isoquinolinyl and hydroxynaphthyl ureas as potent antagonists of the human TRPV1 receptor. The synthesis and Structure-activity relationships (SAR) of the series are described.
MeSH terms
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Binding, Competitive / drug effects
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Cell Line
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Drug Evaluation, Preclinical
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Humans
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Molecular Structure
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Structure-Activity Relationship
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TRPV Cation Channels / antagonists & inhibitors*
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TRPV Cation Channels / chemistry
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TRPV Cation Channels / metabolism*
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Tetrahydronaphthalenes / chemistry
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Tetrahydronaphthalenes / pharmacology*
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Urea / analogs & derivatives
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Urea / chemistry
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Urea / pharmacology*
Substances
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TRPV Cation Channels
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TRPV1 protein, human
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Tetrahydronaphthalenes
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Urea