A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis |
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| Authors: | Brown Dearg S Belfield Andrew J Brown George R Campbell Douglas Foubister Alan Masters David J Pike Kurt G Snelson Wendy L Wells Stuart L |
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| Institution: | AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. dearg.brown@astrazeneca.com |
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| Abstract: | A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues. |
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