Molecules, Vol. 21, Pages 677: Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N´-Diarylurea Derivatives (Molecules)

We have identified a novel series of substituted N,N´-diarylurea p38? inhibitors. The inhibitory activity of the target compounds against the enzyme p38?, MAPKAPK2 in BHK cells, TNF-? release in LPS-stimulated THP-1 cells and p38? binding experiments were tested. Among these compounds, 25a inhibited the p38? enzyme with an IC50 value of 0.47 nM and a KD value of 1.54 × 10-8 and appears to be the most promising one in the series.