Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists

被引：19

作者：

Barnett, Heather A. ^{[2
]}

Coe, Diane M. ^{[2
]}

Cooper, Tony W. J. ^{[2
]}

Jack, Torquil I. ^{[1
]}

Jones, Haydn T. ^{[2
]}

Macdonald, Simon J. F. ^{[2
]}

McLay, Iain M.

Rayner, Natalie ^{[2
]}

Sasse, Rosemary Z.

Shipley, Tracy J. ^{[1
]}

Skone, Phil A. ^{[1
]}

Somers, Graham I. ^{[2
]}

Taylor, Simon ^{[1
]}

Uings, Iain J. ^{[1
]}

Woolven, James M.

Weingarten, Gordon G. ^{[1
]}

机构：

[1] Med Res Ctr, Immunoinflammat CEDD, Stevenage SG1 2NY, Herts, England

[2] Med Res Ctr, Resp CEDD, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 01期

关键词：

GR; Glucocorticoid; Aminopyrazole; A-RING MIMETICS; FLUTICASONE FUROATE; IN-VITRO; BINDING; MODULATORS; EFFICACY;

D O I：

10.1016/j.bmcl.2008.10.128

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compounds with lower lipophilicity, for example N-hydroxyethyl benzamides (e.g., 16e). (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：158 / 162

页数：5

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