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Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds |
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| Authors: | Murali Dhar T G Wrobleski Stephen T Lin Shuqun Furch Joseph A Nirschl David S Fan Yi Todderud Gordon Pitt Sidney Doweyko Arthur M Sack John S Mathur Arvind McKinnon Murray Barrish Joel C Dodd John H Schieven Gary L Leftheris Katerina |
| Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. murali.dhar@bms.com |
| 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. |
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