| Literature DB >> 17664068 |
T G Murali Dhar1, Stephen T Wrobleski, Shuqun Lin, Joseph A Furch, David S Nirschl, Yi Fan, Gordon Todderud, Sidney Pitt, Arthur M Doweyko, John S Sack, Arvind Mathur, Murray McKinnon, Joel C Barrish, John H Dodd, Gary L Schieven, Katerina Leftheris.
Abstract
The synthesis and structure-activity relationships (SAR) of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38alpha MAP kinase with good cellular potency toward the inhibition of TNF-alpha production. X-ray co-crystallography of an oxalamide analog (24) bound to unphosphorylated p38alpha is also disclosed.Entities:
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Year: 2007 PMID： 17664068 DOI： 10.1016/j.bmcl.2007.07.029
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823