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

Autor:	Jie Hu, John J. Perumattam, Joon Jung, Sundeep Dugar, Jocelyn Tabora, Sarvajit Chakravarty, Imad Nashashibi, Qing Lu, Albert Liclican, Daniel E. Levy, Maureen Laney, Xuefei Tan, Gregory R. Luedtke, Ramona Almirez, Richland Tester, Vinh Tran, Babu J. Mavunkel
Rok vydání:	2009
Předmět:	Indoles Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Piperazines Protein Structure Secondary Mitogen-Activated Protein Kinase 14 chemistry.chemical_compound Dogs Pharmacokinetics Drug Discovery Animals Humans Methylene Molecular Biology Piperazine Protein Kinase Inhibitors Indole test chemistry.chemical_classification biology Kinase Organic Chemistry Haplorhini Rats Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 20(3)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab090924b003a47ad9f1dc0b58b36e5e https://pubmed.ncbi.nlm.nih.gov/20071169 Zobrazit plný text záznamu Full Text from ScienceDirect