Structure–activity relationships of triazolopyridine oxazole p38 inhibitors: Identification of candidates for clinical development
Bioorganic & Medicinal Chemistry Letters（2006）
摘要
The synthesis, structure–activity relationship, in vivo activity, and metabolic profile for a series of triazolopyridine-oxazole based p38 inhibitors are described. The deficiencies of the lead structure in the series, CP-808844, were overcome by changes to the C4 aryl group and the triazole side-chain culminating in the identification of several potential clinical candidates.
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关键词
p38 kinase,MAP,Inhibitor,SAR,Clinical candidate,Triazolopyridine,Oxazole,Triazole,TNF-α,CP-808844,Inflammation,Arthritis,Cytokine,Anti-inflammatory
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