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

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• 作者：Subas M. Sakya ; Kristin M. Lundy DeMello ; Martha L. Minich ; Bryson Rast ; Andrei Shavnya ; Robert J. Rafka ; David A. Koss ; Hengmiao Cheng ; Jin Li ; Burton H. Jaynes et al.
• 关键词：Cyclooxygenase ; COX-2 inhibitors ; Canine ; Feline ; Pyrazoles
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 January 2006
• 卷：16
• 期：2
• 页码：288-292
• 文件大小：156 K

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.