| 20071169 |
Tan X, Tester RW, Luedtke GR, Chakravarty S, Mavunkel BJ, Perumattam JJ, Lu Q, Nashashibi I, Jung J, Hu J, Liclican A, Almirez R, Tabora J, Tran V, Laney M, Levy DE, Dugar S: Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2010 Feb 1;20(3):828-31. Epub 2010 Jan 4.
Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38alpha MAP kinase inhibitors are described. Biological evaluation of these compounds focused on maintaining activity while improving pharmacokinetic (PK) properties. Improved properties were observed for structures bearing substitutions on the benzylic methylene. |
32(0,1,1,2) |