The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor
- Hynes, John
- Wu, Hong
- Pitt, Sidney
- Shen, Ding Ren
- Zhang, Rosemary F.
- Schieven, Gary L.
- Gillooly, Kathleen M.
- Shuster, David J.
- Taylor, Tracy L.
- Yang, XiaoXia
- McIntyre, Kim W.
- McKinnon, Murray
- Zhang, Hongjian
- Marathe, Punit H.
- Doweyko, Arthur M.
- Kish, Kevin
- Kiefer, Susan E.
- Sack, John S.
- Newitt, John A.
- Barrish, Joel C.
- Dodd, John H.
- Leftheris, Katerina
Publication date
March 2008
DOI Publisher
Elsevier BV ISSN
0960-894X Citation count (estimate)
18Abstract
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
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