Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles
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- 作者：Xuefei Tan ; Richl ; W. Tester ; Gregory R. Luedtke ; Sarvajit Chakravarty ; Babu J. Mavunkel ; John J. Perumattam ; Qing Lu ; Imad Nashashibi ; Joon Jung ; Jie Hu ; Albert Liclican ; Ramona Almirez ; Jocelyn Tabo
- 关键词：p38 ; MAP ; Kinase ; Inhibitor ; Inflammatory
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：1 February 2010
- 年：2010
- 卷：20
- 期：3
- 页码：828-831
- 全文大小：422 K
文摘
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.