116565-03-8Relevant articles and documents
Synthesis of macrocyclic α-ketoamide as a selective and reversible immunoproteasome inhibitor
Ding, Rui,Wilson, Daniel J.,Chen, Liqiang
, p. 410 - 420 (2021)
In recent years, the human immunoproteasome has emerged as an attractive therapeutic target for various diseases, leading to a growing interest in the discovery of immunoproteasome inhibitors that selectively target specific subunits. Herein we report the design, synthesis, and evaluation of a new immunoproteasome inhibitor that feature a macrocyclic ring containing an internal α-ketoamide warhead. This compound is a selective and reversible inhibitor of immunoproteasome subunits β1i and β5i and shows essentially no inhibition of constitutive proteasome subunits. [Figure not available: see fulltext.]
Process for reducing α-amino ketones
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, (2008/06/13)
The present invention has its objects to provide a method for reducing α-aminoketone derivatives under mild conditions with high stereoselectivity. This invention is a method for reducing α-aminoketone which comprises reacting an a-aminoketone derivative of general formula (1) with a compound prepared from an organoaluminum compound of general formula (4), a sulfonic acid derivative of general formula (5), and an alcohol compound of general formula (6) to give an α-aminoalcohol derivative of general formula (7)
Development of selective tight-binding inhibitors of leukotriene A4 hydrolase
Yuan,Munoz,Wong,Haeggstrom,Wetterholm,Samuelsson
, p. 211 - 220 (2007/10/02)
Leukotriene A4 hydrolase is a zinc-containing enzyme which exhibits both epoxide hydrolase and aminopeptidase activities. Since the enzyme product leukotriene B4 is an inflammatory mediator, it is of interest to develop selective inh