Development of triarylsulfonamides as novel anti-inflammatory agents

Iain R. Greig, Emmanuel Coste, Stuart H. Ralston, Robert J. van 't Hof

Research output: Contribution to journalArticlepeer-review

Abstract / Description of output

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

Original languageEnglish
Pages (from-to)816-820
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Issue number3
Publication statusPublished - 1 Feb 2013


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