3-acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists

Authors
Lee, J Park, SU Kim, JY Kim, JK Lee, J Oh, U Marquez, VE Beheshti, M Wang, QJ Modarres, S Blumberg, PM
Citation
J. Lee et al., 3-acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists, BIOORG MED, 9(20), 1999, pp. 2909-2914
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
20
Year of publication
1999
Pages
2909 - 2914
Database
ISI
SICI code
0960-894X(19991018)9:20<2909:3AAEOH>2.0.ZU;2-D
Abstract
A series of 3-acyloxy-2-phenalkylpropyl amides and eaters of homovanillic a cid were designed and synthesized as vanilloid receptor agonists containing the three principal pharmacophores of resiniferatoxin. Amide analogues 23, 5 and II were found to be potent agonists in vanilloid receptor assay both for ligand binding and for activation. (C) 1999 Elsevier Science Ltd. All rights reserved.