215941-02-9Relevant articles and documents
Synthesis and evaluation of 5-fluoro-2-aryloxazolo[5,4- b ]pyridines as β-amyloid PET ligands and identification of MK-3328
Harrison, Scott T.,Mulhearn, James,Wolkenberg, Scott E.,Miller, Patricia J.,O'Malley, Stacey S.,Zeng, Zhizhen,Williams Jr., David L.,Hostetler, Eric D.,Sanabria-Bohorquez, Sandra,Gammage, Linda,Fan, Hong,Sur, Cyrille,Culberson, J. Christopher,Hargreaves, Richard J.,Cook, Jacquelynn J.,Hartman, George D.,Barrow, James C.
supporting information; experimental part, p. 498 - 502 (2011/09/14)
5-Fluoro-2-aryloxazolo[5,4-b]pyridines were synthesized and investigated as potential 18F containing β-amyloid PET ligands. In competition binding assays using human AD brain homogenates, compounds 14b, 16b, and 17b were identified as having favorable potency versus human β-amyloid plaque and were radiolabeled for further evaluation in in vitro binding and in vivo PET imaging experiments. These studies led to the identification of 17b (MK-3328) as a candidate PET ligand for the clinical assessment of β-amyloid plaque load.
