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The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)—A potent and efficacious p38α MAP kinase inhibitor

2008; Elsevier BV; Volume: 18; Issue: 6 Linguagem: Inglês

10.1016/j.bmcl.2008.02.031

1464-3405

John Hynes, Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang, Gary L. Schieven, Kathleen M. Gillooly, David J. Shuster, Tracy L. Taylor, Xiao-Xia Yang, Kim W. McIntyre, Murray McKinnon, Hongjian Zhang, Punit H. Marathe, Arthur M. Doweyko, Kevin Kish, Susan E. Kiefer, John S. Sack, John A. Newitt, Joel C. Barrish, John H. Dodd, Katerina Leftheris,

Synthesis and biological activity

A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.