Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors

被引：35

作者：

Beswick, P ^{[1
]}

Bingham, S ^{[1
]}

Bountra, C ^{[1
]}

Brown, T ^{[1
]}

Browning, K ^{[1
]}

Campbell, I ^{[1
]}

Chessell, I ^{[1
]}

Clayton, N ^{[1
]}

Collins, S ^{[1
]}

Corfield, J ^{[1
]}

Guntrip, S ^{[1
]}

Haslam, C ^{[1
]}

Lambeth, P ^{[1
]}

Lucas, F ^{[1
]}

Mathews, N ^{[1
]}

Murkit, G ^{[1
]}

Naylor, A ^{[1
]}

Pegg, N ^{[1
]}

Pickup, E ^{[1
]}

Player, H ^{[1
]}

Price, H ^{[1
]}

Stevens, A ^{[1
]}

Stratton, S ^{[1
]}

Wiseman, J ^{[1
]}

机构：

[1] GlaxoSmithKline, Neurol & Gastrointest Dis Ctr Excellence Durg Dis, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 21期

关键词：

D O I：

10.1016/j.bmcl.2004.07.089

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

GW406381 (8), currently undergoing clinical evaluation for the treatment of inflammatory pain is a member of a novel series of 2,3-diaryl-pyrazolo[1,5-b]pyridazine based cyclooxygenase-2 (COX-2) inhibitors, which have been shown to be highly potent and selective. Several examples of the series, in addition to possessing favourable pharmacokinetic profiles and analgesic activity in vivo, have also demonstrated relatively high brain penetration in the rat compared with the clinically available compounds, which may ultimately prove beneficial in the treatment of pain. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5445 / 5448

页数：4

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