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Pubmed ID :14561090
Publication Date : //

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


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)-1H-pyrrolo[3,2-b] pyridine, is described. X-ray crystallographic data of the lead bound to the active site of p38 was used to guide the optimization of the series. Specific focus was placed on modulating the physical properties of the core while maintaining potent inhibition of p38. These efforts identified 42c as a potent inhibitor of p38, which also possessed the required physical properties worthy of advanced studies.

Authors : 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 ,

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