Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds

被引：23

作者：

Dhar, T. G. Murali ^{[1
]}

Wrobleski, Stephen T. ^{[1
]}

Lin, Shuqun ^{[1
]}

Furch, Joseph A. ^{[1
]}

Nirschl, David S. ^{[1
]}

Fan, Yi ^{[1
]}

Todderud, Gordon ^{[1
]}

Pitt, Sidney ^{[1
]}

Doweyko, Arthur M. ^{[1
]}

Sack, John S. ^{[1
]}

Mathur, Arvind ^{[1
]}

McKinnon, Murray ^{[1
]}

Barrish, Joel C. ^{[1
]}

Dodd, John H. ^{[1
]}

Schieven, Gary L. ^{[1
]}

Leftheris, Katerina ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 18期

关键词：

p38; alpha; MAP kinase inhibitors; TNF alpha; X-ray co-crystallography;

D O I：

10.1016/j.bmcl.2007.07.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and structure-activity relationships (SAR) of p38 alpha MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38a 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 p38 alpha is also disclosed. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5019 / 5024

页数：6

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