- Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Bioorganic & medicinal chemistry letters (2008-03-18)
Hui Huang, Daniel A Hutta, Huaping Hu, Renee L DesJarlais, Carsten Schubert, Ioanna P Petrounia, Margery A Chaikin, Carl L Manthey, Mark R Player
PMID18342505
摘要
A series of pyrimidinopyridones has been designed, synthesized and shown to be potent and selective inhibitors of the FMS tyrosine kinase. Introduction of an amide substituent at the 6-position of the pyridone core resulted in a significant potency increase. Compound 24 effectively inhibited in vivo LPS-induced TNF in mice greater than 80%.
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