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ID: ALA1132910
Journal: Bioorg Med Chem Lett
Title: SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.
Authors: Revesz L, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Zimmerlin AG.
Abstract: 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.
CiteXplore: 10866395