Author/Authors :
T.G. Murali Dhar، نويسنده , , Stephen T. Wrobleski، نويسنده , , Shuqun Lin، نويسنده , , Joseph A. Furch، نويسنده , , David S. Nirschl، نويسنده , , Yi Fan، نويسنده , , Gordon Todderud، نويسنده , , Sidney Pitt، نويسنده , , Arthur M. Doweyko، نويسنده , , John S. Sack، نويسنده , , Arvind Mathur، نويسنده , , Murray McKinnon، نويسنده , , Joel C. Barrish، نويسنده , , John H. Dodd، نويسنده , , Gary L. Schieven، نويسنده , , Katerina Leftheris، نويسنده ,
Abstract :
The synthesis and structure–activity relationships (SAR) of p38α MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38α MAP kinase with good cellular potency toward the inhibition of TNF-α production. X-ray co-crystallography of an oxalamide analog (24) bound to unphosphorylated p38α is also disclosed.
Keywords :
X-ray co-crystallography , TNF? , p38? , MAP kinase inhibitors
