| Literature DB >> 14698197 |
Mark E McDonnell1, Sui Po Zhang, Nadia Nasser, Adrienne E Dubin, Scott L Dax.
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.Entities:
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Year: 2004 PMID： 14698197 DOI： 10.1016/j.bmcl.2003.09.090
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823