3-(2-methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors

被引：49

作者：

Ranatunge, RR ^{[1
]}

Earl, RA ^{[1
]}

Garvey, DS ^{[1
]}

Janero, DR ^{[1
]}

Letts, LG ^{[1
]}

Martino, AM ^{[1
]}

Murty, MG ^{[1
]}

Richardson, SK ^{[1
]}

Schwalb, DJ ^{[1
]}

Young, DV ^{[1
]}

Zemtseva, IS ^{[1
]}

机构：

[1] NtroMed Inc, Lexington, MA 02421 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 24期

关键词：

cyclooxygenase-2 (COX-2); pyrazole; tetrahydrofuran-2-yl;

D O I：

10.1016/j.bmcl.2004.09.073

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-(2-methoxytetrahydrofuran-2-yl)pyrazoles (4-10) was synthesized. The compounds were evaluated for their ability to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) activity in human whole blood (HWB). The compound, 5-(4-methanesulfotiylphenyl)-3-(2-methoxytetrahydrofuran-2-yl)-1-p-tolyl-1H-pyrazole 5 showed potent and selective COX-2 inhibition (IC50 for COX-1: >100 muM and COX-2: 1.2 muM). (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：6049 / 6052

页数：4

共 19 条

[1]

BANDARAGE RR, 2002, 224 ACS NAT M BOST M

[2]

Catella-Lawson Francesca, 2001, American Journal of Medicine, V110, p28S

[3] Prevention of thrombosis and vascular inflammation: benefits and limitations of selective or combined COX-1, COX-2 and 5-LOX inhibitors [J].