1,4-Diazepane-2-ones as novel inhibitors of LFA-1

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• 作者：Wattanasin ; Sompong ; Albert ; Rainer ; Ehrhardt ; Claus ; Roche ; Didier ; Sabio ; Michael ; Hommel ; Ulrich ; 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：499-502
• 全文大小：240 K

文摘

The design, synthesis, and biological evaluation of 1,4-diazepane-2-ones as novel LFA-1 antagonists from a scaffold-based combinatorial library are described. Initial optimization of the library lead has resulted in high-affinity antagonists of the LFA-1/ICAM-1 interaction, such as compounds 18d and 18e with IC₅₀ values of 110 and 70nM, respectively.