2. Academic Validation
  3. Design and synthesis of piperazine-indole p38 alpha MAP kinase inhibitors with improved pharmacokinetic profiles

Design and synthesis of piperazine-indole p38 alpha MAP kinase inhibitors with improved pharmacokinetic profiles

  • Bioorg Med Chem Lett. 2010 Feb 1;20(3):828-31. doi: 10.1016/j.bmcl.2009.12.091.
Xuefei Tan 1,  Richland 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 Tabora,  Vinh Tran,  Maureen Laney,  Daniel E Levy,  Sundeep Dugar
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry and Biology, Scios inc, 6500 Paseo Padre Parkway, Fremont, CA 94555, United States. [email protected]
PMID: 20071169 DOI: 10.1016/j.bmcl.2009.12.091
Abstract

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.

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