N-Pyridin-3-yl- and N-quinolin-3-yl-benzamides: Modulators of Human Vanilloid Receptor 1 (TRPV1)

High throughput screening of our compound library revealed a series of N-pyridyl-3-benzamides as low micromolar agonists of the human TRPV1 receptor. Synthesis of analogs in this series led to the discovery of a series of N-quinolin-3-yl-benzamides as low nanomolar antagonists of human TRPV1.

Graphical abstractThe synthesis and biological activity of a series of 3-quinolinyl p-aminobenzamide TRPV1 antagonists are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide