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 language | English |
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Pages (from-to) | 816-820 |
Number of pages | 5 |
Journal | Bioorganic & Medicinal Chemistry Letters |
Volume | 23 |
Issue number | 3 |
Early online date | 27 Dec 2012 |
DOIs | |
Publication status | Published - Feb 2013 |
Keywords
- TNF-a
- NFκB
- inflammation
- rheumatoid arthritis
- bone loss
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Discovery and commercialisation of new drug for rheumatoid arthritis and related conditions
Iain Greig (Coordinator), Stuart Ralston (Coordinator) & Rob. J. van't Hof (Coordinator)
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