Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors
Bioorganic & Medicinal Chemistry Letters(2010)
摘要
During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were prepared and evaluated in an attempt to also improve the cardiovascular safety profile over lead arylamide 1, which possessed ion channel activity. The resultant compounds retained excellent potency and exhibited diminished ion channel activity.
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关键词
FMS,CSF-1R,M-CSF,Colony stimulating factor-1,Macrophages,Anti-inflammatory activity
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