Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists

被引：18

作者：

Lee, J ^{[1
]}

Kang, SU

Kil, MJ

Shin, M

Lim, JO

Choi, HK

Jin, MK

Kim, SY

Kim, SE

Lee, YS

Min, KH

Kim, YH

Ha, HJ

Tran, R

Welter, JD

Wang, Y

Szabo, T

Pearce, LV

Lundberg, DJ

Toth, A

Pavlyukovets, VA

Morgan, MA

Blumberg, PM

机构：

[1] Seoul Natl Univ, Coll Pharm, Pharmaceut Sci Res Inst, Seoul 151742, South Korea

[2] Digitalbiotech, Ansan 425839, Kyounggi Do, South Korea

[3] NCI, Cellular Carcinogenesis & Tumor Promot Lab, Canc Res Ctr, NIH, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 18期

关键词：

TRPV1; antagonist; vanilloid receptor 1 antagonist; capsaicin; resiniferatoxin;

D O I：

10.1016/j.bmcl.2005.06.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N '-[4-(methylsulfonylamino)benzyl]thio-urea analogues have been investigated as TRPV1 receptor antagonists. The 2-halogen analogues showed enhanced antagonism compared to the prototype antagonist. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4136 / 4142

页数：7

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