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

[摘要]：5-Fluoro-2-aryloxazolo[5,4-b]pyridines were synthesized and investigated as potential (18)F containing beta-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 beta-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 beta-amyloid plaque load.

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