Development of triarylsulfonamides as novel anti-inflammatory agents.
Basic Information
ID: ALA2321720
Journal: Bioorg Med Chem Lett
Title: Development of triarylsulfonamides as novel anti-inflammatory agents.
Authors: Greig IR, Coste E, Ralston SH, van 't Hof RJ.
Abstract: 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 <100 nM against J774 macrophages and osteoclasts, but with little activity against osteoblasts or hepatocytes (IC(50) >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.
CiteXplore: 23265887
DOI: 10.1016/j.bmcl.2012.11.067
Patent ID: ┄