Details

Autor(en) / Beteiligte

• REVESZ, L
• DI PADOVA, F. E
• BUHL, T
• FEIFEL, R
• GRAM, H
• HIESTAND, P
• MANNING, U
• ZIMMERLIN, A. G

Titel

SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2000-06, Vol.10 (11), p.1261-1264

Ort / Verlag

Oxford: Elsevier

Erscheinungsjahr

2000

Link zum Volltext

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• The 4-hydroxypiperidine substituent was found to confer high p38 selectivity devoid of COX-1 affinity, when attached to a series of pyridinyl substituted heterocycles. Pyridinyloxazole 11 showed a promising in vivo profile with bioavailability of 64% and ED50 in rat collagen induced arthritis of 10 mg/kg po bid. In contrast to pyridinylimidazoles such as SB 203580, 11 did not inhibit human cytochrome P450 isoenzymes.