5-heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers

被引：36

作者：

Sakya, SM ^{[1
]}

Cheng, HM ^{[1
]}

DeMello, KML ^{[1
]}

Shavnya, A ^{[1
]}

Minich, ML ^{[1
]}

Rast, B ^{[1
]}

Dutra, J ^{[1
]}

Li, C ^{[1
]}

Rafka, RJ ^{[1
]}

Koss, DA ^{[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
]}

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 / 05期

关键词：

pyrazoles; heteroatom; COX-1; COX-2; aanine; SAR;

D O I：

10.1016/j.bmcl.2005.11.110

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alky](thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine whole blood, (CWB) COX-2 assay. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1202 / 1206

页数：5

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