Synthesis and biological evaluation of pyridazinone analogues as potential cardiac positron emission tomography tracers

A Purohit, H Radeke, M Azure, K Hanson…

文献索引：Purohit, Ajay; Radeke, Heike; Azure, Michael; Hanson, Kelley; Benetti, Richard; Su, Fran; Yalamanchili, Padmaja; Yu, Ming; Hayes, Megan; Guaraldi, Mary; Kagan, Mikhail; Robinson, Simon; Casebier, David Journal of Medicinal Chemistry, 2008 , vol. 51, # 10 p. 2954 - 2970

全文：HTML全文

被引用次数: 32

摘要

A series of fluorinated pyridazinone derivatives with IC50 values ranging from 8 to 4000 nM for the mitochondrial complex 1 (MC1) have been prepared. Structure–activity relationship (SAR) assessment indicated preference of the fluorine label to be incorporated on an alkyl side chain rather than directly on the pyridazinone moiety. Tissue distribution studies of a series of analogues ([18F] 22–28) in Sprague− Dawley (SD) rats identified [18F] 27 as the ...