1222508-86-2Relevant academic research and scientific papers
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.
BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
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Page/Page column 108, (2011/02/24)
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds are of the following formula: wherein R1 is a member selected from alkyl or aryl or heteroaryl, in which at least one substituent on said alkyl or said aryl or said heteroaryl is optionally substituted with a member selected from halogen, C1 or C2 or C3 or C4 or C5 or C6 unsubstituted alkyl, C1 or C2 or C3or C4 or C5 or C6 unsubstituted alkoxy, halosubstituted C1 or C2 or C3or C4 or C5 or C6 alkyl, halosubstituted C1 or C2 or C3 or C4 or C5 or C6 alkoxy, unsubstituted C1 or C2 or C3 or C4or C5 or C6 alkylthio, unsubstituted phenyl; and X is aryl or heteroaryl, in which one substituent on said aryl or said heteroaryl is a member selected from halogen, unsubstituted C1 or C2 or C3 or C4 or C5 or C6 alkyl, unsubstituted C1 or C2 or C3 or C4 or C5 or C6 alkoxy, halosubstituted C1 or C2 or C3 or C4 or C5 or C6 alkyl, halosubstituted C1 or C2 or C3 or C4 or C5 or C6 alkoxy, unsubstituted C1 or C2 or C3 or C4 or C5 or C6 alkylthio, unsubstituted phenyl or a salt thereof.
BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS
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Page/Page column 101, (2010/04/30)
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
