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

被引：17

作者：

Lee, J ^{[1
]}

Park, SU

Kim, JY

Kim, JK

Lee, J ^{[1
]}

Oh, U

Marquez, VE

Beheshti, M

Wang, QJ

Modarres, S

Blumberg, PM

机构：

[1] Seoul Natl Univ, Coll Pharm, Labs Med Chem, Kwanak Ku, Seoul 151742, South Korea

[2] Seoul Natl Univ, Coll Pharm, CRI, Sensory Res Grp,Kwanak Ku, Seoul 151742, South Korea

[3] NCI, Med Chem Lab, Div Basic Sci, NIH, Bethesda, MD 20892 USA

[4] NCI, Lab Cellular Carcinogenesis & Tumor Promot, Div Basic Sci, NIH, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(99)00513-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid 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.

引用

页码：2909 / 2914

页数：6

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