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Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.

Jetter, Michele C; Youngman, Mark A; McNally, James J; McDonnell, Mark E; Zhang, Sui-Po; Dubin, Adrienne E; Nasser, Nadia; Codd, Ellen E; Flores, Christopher M; Dax, Scott L.

Bioorg Med Chem Lett ; 17(22): 6160-3, 2007 Nov 15.

Article in English | MEDLINE | ID: mdl-17892935

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.

Subject(s)

TRPV Cation Channels/antagonists & inhibitors , TRPV Cation Channels/metabolism , Tetrahydronaphthalenes/pharmacology , Urea/pharmacology , Binding, Competitive/drug effects , Cell Line , Drug Evaluation, Preclinical , Humans , Molecular Structure , Structure-Activity Relationship , TRPV Cation Channels/chemistry , Tetrahydronaphthalenes/chemistry , Urea/analogs & derivatives , Urea/chemistry

ABSTRACT

Subject(s)

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