2. Academic Validation
  3. 7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1

7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1

  • Bioorg Med Chem Lett. 2004 Jan 19;14(2):531-4. doi: 10.1016/j.bmcl.2003.09.090.
Mark E McDonnell 1,  Sui Po Zhang,  Nadia Nasser,  Adrienne E Dubin,  Scott L Dax
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA.
PMID: 14698197 DOI: 10.1016/j.bmcl.2003.09.090
Abstract

A series of structurally simple 7-hydroxynaphthalenyl ureas and amides were discovered to be potent ligands of human vanilloid receptor 1 (VR1). 1-(7-Hydroxynaphthalen-1-yl)-3-(4-trifluoromethylbenzyl)urea 5f exhibited nanomolar binding affinity (K(i)=1.0nM) and upon capsaicin challenge, behaved as a potent functional antagonist (IC(50)=4nM). The synthesis and structure-activity relationships (SARs) for the series are described.

Figures