N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1

Michele C Jetter; Mark A Youngman; James J McNally; Sui-Po Zhang; Adrienne E Dubin; Nadia Nasser; Scott L Dax

doi:10.1016/j.bmcl.2004.04.038

N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3053-6. doi: 10.1016/j.bmcl.2004.04.038.

Authors

Michele C Jetter¹, Mark A Youngman, James J McNally, Sui-Po Zhang, Adrienne E Dubin, Nadia Nasser, Scott L Dax

Affiliation

¹ Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA.

PMID: 15149643
DOI: 10.1016/j.bmcl.2004.04.038

Abstract

Starting from a low micromolar agonist lead identified by high-throughput screening, series of N-isoquinolin-5-yl-N'-aralkyl ureas and analogous amides were developed as potent antagonists of human vanilloid receptor 1 (VR1). The synthesis and structure-activity relationships (SAR) of the series are described.

MeSH terms

Amides / chemistry*
Amides / metabolism
Cell Line
Humans
Isoquinolines / chemistry*
Isoquinolines / metabolism
Receptors, Drug / antagonists & inhibitors*
Receptors, Drug / metabolism
TRPV Cation Channels
Urea / chemistry*
Urea / metabolism

Substances

Amides
Isoquinolines
Receptors, Drug
TRPV Cation Channels
TRPV1 receptor
Urea