Heteroaryl β-tetralin ureas as novel antagonists of human TRPV1

We report on a series of α-substituted-β-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.

The synthesis and biological activity of a series of aminotetralin-derived heteroaryl urea TRPV1 antagonists is reported.Figure optionsDownload as PowerPoint slide