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.
Collis
A J
AJ
Aventis Pharma, Dagenham Research Centre, Essex, UK.
Foster
M L
ML
Halley
F
F
Maslen
C
C
McLay
I M
IM
Page
K M
KM
Redford
E J
EJ
Souness
J E
JE
Wilsher
N E
NE
D000704:Analysis of Variance; D000818:Animals; D019540:Area Under Curve; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D002478:Cells, Cultured; D065607:Cytochrome P-450 Enzyme Inhibitors; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D008297:Male; D051379:Mice; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*; D011897:Random Allocation; D051381:Rats; D011917:Rats, Inbred Lew; D011994:Recombinant Proteins / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism; D048051:p38 Mitogen-Activated Protein Kinases
D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D008070:Lipopolysaccharides; D011743:Pyrimidines; C432548:RPR 203494; D011994:Recombinant Proteins; D014409:Tumor Necrosis Factor-alpha; D020928:Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases