Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles

…, J Jung, J Hu, A Liclican, R Almirez, J Tabora…

文献索引：Tan, Xuefei; Tester, Richland W.; Luedtke, Gregory R.; Chakravarty, Sarvajit; Mavunkel, Babu J.; Perumattam, John J.; Lu, Qing; Nashashibi, Imad; Jung, Joon; Hu, Jie; Liclican, Albert; Almirez, Ramona; Tabora, Jocelyn; Tran, Vinh; Laney, Maureen; Levy, Daniel E.; Dugar, Sundeep Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 828 - 831

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被引用次数: 8

摘要

Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38α 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.