2. Academic Validation
  3. N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1

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.
Michele C Jetter 1,  Mark A Youngman,  James J McNally,  Sui-Po Zhang,  Adrienne E Dubin,  Nadia Nasser,  Scott L Dax
Affiliations

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.

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