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Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase

…, J Freire-Moar, J Lim, J Mcintosh, J Miller…

文献索引:Trejo, Alejandra; Arzeno, Humberto; Browner, Michelle; Chanda, Sushmita; Cheng, Soan; Comer, Daniel D.; Dalrymple, Stacie A.; Dunten, Pete; Lafargue, JoAnn; Lovejoy, Brett; Freire-Moar, Jose; Lim, Julie; McIntosh, Joel; Miller, Jennifer; Papp, Eva; Reuter, Deborah; Roberts, Rick; Sanpablo, Florentino; Saunders, John; Song, Kyung; Villasenor, Armando; Warren, Stephen D.; Welch, Mary; Weller, Paul; Whiteley, Phyllis E.; Zeng, Lu; Goldstein, David M. Journal of Medicinal Chemistry, 2003 , vol. 46, # 22 p. 4702 - 4713

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被引用次数: 86

摘要

Inhibition of the biosynthesis of proinflammatory cytokines such as tumor necrosis factor and interleukin-1 via p38 has been an approach toward the development of a disease modifying agent for the treatment of chronic inflammation and autoimmune diseases. The development of a new core structure of p38 inhibitors, 3-(4-fluorophenyl)-2-(pyridin-4-yl)-1 H-pyrrolo [3, 2- b] pyridine, is described. X-ray crystallographic data of the lead bound to the active site of ...