RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency

Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst them, RPR203494 was identified with a better in vitro profile than RPR200765A. Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst t...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-03, Vol.11 (5), p.693-696
Hauptverfasser:	Collis, Alan J, Foster, Martyn L, Halley, Frank, Maslen, Christopher, McLay, Iain M, Page, Kenneth M, Redford, E.Jane, Souness, John E, Wilsher, Nicola E
Format:	Artikel
Sprache:	eng
Schlagworte:	Analysis of Variance Animals Area Under Curve Arthritis, Rheumatoid - drug therapy Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cells, Cultured Cytochrome P-450 Enzyme Inhibitors Dose-Response Relationship, Drug Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Humans Lipopolysaccharides - pharmacology Male Medical sciences Mice Mitogen-Activated Protein Kinases - antagonists & inhibitors Mitogen-Activated Protein Kinases - metabolism Molecular Structure Monocytes - drug effects Monocytes - metabolism p38 Mitogen-Activated Protein Kinases Pharmacology. Drug treatments Pyrimidines - chemistry Pyrimidines - pharmacology Random Allocation Rats Rats, Inbred Lew Recombinant Proteins - metabolism Tumor Necrosis Factor-alpha - metabolism
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Zusammenfassung:	Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst them, RPR203494 was identified with a better in vitro profile than RPR200765A. Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst them, RPR203494 was identified with a better in vitro profile than RPR200765A.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00034-8