Development of triarylsulfonamides as novel anti-inflammatory agents

IR Greig, E Coste, SH Ralston, RJ van't Hof

文献索引：Greig, Iain R.; Coste, Emmanuel; Ralston, Stuart H.; Van 'T Hof, Robert J. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 3 p. 816 - 820

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被引用次数: 5

摘要

Triaylsulfonamides were identified as novel anti-inflammatory agents, acting by inhibition of RANKL and TNFα signaling. Structure-activity studies led to the identification of compounds with in vitro potencies of< 100nM against J774 macrophages and osteoclasts, but with little activity against osteoblasts or hepatocytes (IC50> 50μM). A representative compound (4k, ABD455) was able to completely prevent inflammation in vivo in a prevention model and ...