Title of article
Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
5019
To page
5024
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798545
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