5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog

被引：48

作者：

Sakya, SM ^{[1
]}

Demello, KML ^{[1
]}

Minich, ML ^{[1
]}

Rast, B ^{[1
]}

Shavnya, A ^{[1
]}

Rafka, RJ ^{[1
]}

Koss, DA ^{[1
]}

Cheng, HM ^{[1
]}

Li, J ^{[1
]}

Jaynes, BH ^{[1
]}

Ziegler, CB ^{[1
]}

Mann, DW ^{[1
]}

Petras, CF ^{[1
]}

Seibel, SB ^{[1
]}

Silvia, AM ^{[1
]}

George, DM ^{[1
]}

Lund, LA ^{[1
]}

St Denis, S ^{[1
]}

Hickman, A ^{[1
]}

Haven, ML ^{[1
]}

Lynch, MP ^{[1
]}

机构：

[1] Pfizer Inc, Vet Med Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 02期

关键词：

cyclooxygenase; COX-2; inhibitors; canine; feline; pyrazoles;

D O I：

10.1016/j.bmcl.2005.10.006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO2Me)/sulfamoyl (SO2NH2)-pyridine derivatives for canine COX enzymes are described. The studies led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：288 / 292

页数：5

共 27 条

[1] GASTROINTESTINAL DAMAGE ASSOCIATED WITH THE USE OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS [J].