Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase

Autor:	Alan G. Benson, John E. Baldus, Michael Hepperle, Li Xing, Kevin D. Jerome, Shaun R. Selness, John K. Walker, Rajesh V. Devraj
Rok vydání:	2010
Předmět:	Molecular model Stereochemistry p38 mitogen-activated protein kinases Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Mitogen-Activated Protein Kinase 14 Structure-Activity Relationship Anti-Infective Agents Drug Discovery Computer Simulation Molecular Biology Protein Kinase Inhibitors chemistry.chemical_classification Binding Sites biology Kinase Organic Chemistry Pyridazines Enzyme chemistry Enzyme inhibitor Mitogen-activated protein kinase Benzene derivatives biology.protein Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 20(10)
ISSN:	1464-3405
Popis:	The synthesis, structure–activity relationship and modeling of a series of 5-substituted-N-aryl pyridazinone based p38α inhibitors are described. In comparing the series to the similar N-aryl pyridinone series, it was found that the pyridazinones maintained a weaker interaction to the p38 enzyme, and therefore showed generally weaker binding than the pyridinones.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f89beae325fb9ce985dc7c72822c83ce https://pubmed.ncbi.nlm.nih.gov/20395140 Zobrazit plný text záznamu Full Text from ScienceDirect