Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors

被引：38

作者：

Cheng, HM ^{[1
]}

DeMello, KML

Li, J

Sakya, SM

Ando, K

Kawamura, K

Kato, T

Rafka, RJ

Jaynes, BH

Ziegler, CB

Stevens, R

Lund, LA

Mann, DW

Kilroy, C

Haven, ML

Nimz, EL

Dutra, JK

Li, C

Minich, ML

Kolosko, NL

Petras, C

Silvia, AM

Seibel, SB

机构：

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

[2] Pfizer Inc, Nagoya Labs, Global Res & Dev, Aichi 4702393, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 08期

关键词：

Cox-2; inhibitor; anti-inflammation; pain; dog;

D O I：

10.1016/j.bmcl.2006.01.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure-activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a canine whole blood COX-2 inhibitory IC50 Of 12 nM and selectivity ratio of COX-1/COX-2 greater than 4000-fold. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2076 / 2080

页数：5

共 23 条

[1]

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