Document Report Card

ID: ALA2203090

Journal: ACS Med Chem Lett

Title: Synthesis and Evaluation of 5-Fluoro-2-aryloxazolo[5,4-b]pyridines as β-Amyloid PET Ligands and Identification of MK-3328.

Authors: Harrison ST, Mulhearn J, Wolkenberg SE, Miller PJ, O'Malley SS, Zeng Z, Williams DL, Hostetler ED, Sanabria-Bohórquez S, Gammage L, Fan H, Sur C, Culberson JC, Hargreaves RJ, Cook JJ, Hartman GD, Barrow JC.

Abstract: 5-Fluoro-2-aryloxazolo[5,4-b]pyridines were synthesized and investigated as potential (18)F 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.

CiteXplore: 24900338

DOI: 10.1021/ml200018n