501906-54-3Relevant academic research and scientific papers
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)
Lin, Songnian,Lombardo, Matthew,Malkani, Sunita,Hale, Jeffrey J.,Mills, Sander G.,Chapman, Kevin,Thompson, James E.,Zhang, Wen Xiao,Wang, Ruixiu,Cubbon, Rose M.,O'Neill, Edward A.,Luell, Silvi,Carballo-Jane, Ester,Yang, Lihu
scheme or table, p. 3238 - 3242 (2010/05/02)
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas are described as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). These compounds demonstrate potent in vitro activity against the enzyme with IC50 values as low as 15 nM, and suppress expression of TNFα in THP-1 cells and in vivo in an acute inflammation model in mice. The synthesis, structure-activity relationship (SAR), and biological evaluation of these compounds are discussed.
