Development of triarylsulfonamides as novel anti-inflammatory agents

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

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Triaylsulfonamides were identified as novel anti-inflammatory agents, acting by inhibition of RANKL and TNFa 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 µM). 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
Volume23
Issue number3
Early online date27 Dec 2012
DOIs
Publication statusPublished - Feb 2013

Keywords

  • TNF-a
  • NFκB
  • inflammation
  • rheumatoid arthritis
  • bone loss

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