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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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 11; no. 5; pp. 693 - 696
Main Authors:	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:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 12-03-2001 Elsevier
Subjects:	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 Imidazole derivatives Five membered ring Cyclopropane derivatives Rat Nitrogen heterocycle Oxygen heterocycle Morpholine derivatives Structure activity relation Area under the curve Six membered ring Chemical synthesis Dioxane derivatives Enzyme Transferases Rodentia Antiinflammatory agent Cytokine Oral administration Enzyme inhibitor Bioavailability In vitro In vivo Vertebrata Mammalia Protein kinase Animal Carboxamide Pyrimidine derivatives Fluorine Organic compounds Pharmacokinetics
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Summary:	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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00034-8