1222509-19-4Relevant articles and documents
Discovery and structure-activity relationships of 6-(benzoylamino) benzoxaboroles as orally active anti-inflammatory agents
Akama, Tsutomu,Dong, Chen,Virtucio, Charlotte,Freund, Yvonne R.,Chen, Daitao,Orr, Matthew D.,Jacobs, Robert T.,Zhang, Yong-Kang,Hernandez, Vincent,Liu, Yang,Wu, Anne,Bu, Wei,Liu, Liang,Jarnagin, Kurt,Plattner, Jacob J.
, p. 5870 - 5873 (2013/10/22)
Structure-activity relationships of 6-(benzoylamino)benzoxaborole analogs were investigated for the inhibition of TNF-α, IL-1β, and IL-6 from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compound 1q showed potent activity against all three cytokines with IC50 values between 0.19 and 0.50 μM, inhibited LPS-induced TNF-α and IL-6 elevation in mice and improved collagen-induced arthritis in mice. Compound 1q (AN4161) is considered to be a promising lead for novel anti-inflammatory agent with an excellent pharmacokinetic profile.