250682-06-5Relevant articles and documents
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
Brown, Dearg S.,Belfield, Andrew J.,Brown, George R.,Campbell, Douglas,Foubister, Alan,Masters, David J.,Pike, Kurt G.,Snelson, Wendy L.,Wells, Stuart L.
, p. 5383 - 5387 (2007/10/03)
The discovery, rational analogue design, synthesis and SAR of a novel bisamide class of p38 MAP kinase inhibitor are reported. The activity in vitro is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues, such as 18. A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38α enzyme activity and lipopolysaccharide-induced tumour necrosis factor-α release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.
