Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors |
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| Authors: | Huang Hui Hutta Daniel A Hu Huaping DesJarlais Renee L Schubert Carsten Petrounia Ioanna P Chaikin Margery A Manthey Carl L Player Mark R |
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| Institution: | Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, Spring House, PA 19477, USA. |
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| Abstract: | 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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