p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones

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• 作者：Hunt ; Julianne A. ; Kallashi ; Florida ; Ruzek ; Rowena D. ; Sinclair ; Peter J. ; Ita ; Ida ; McCormick ; Sherrie X. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2003
• 出版时间：February 10, 2003
• 年：2003
• 卷：13
• 期：3
• 页码：467-470
• 全文大小：182 K

文摘

We have synthesized a series of C7-piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones that are highly potent inhibitors of both p38MAP kinase activity and TNF-α release. The 4-aminopentamethylpiperidine naphthyridinone 5, which was designed to block metabolism at major ‘hot spots’, combined excellent inhibitory potency with good oral bioavailability in the rat.