Abstract
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.
Original language | English (US) |
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Pages (from-to) | 498-502 |
Number of pages | 5 |
Journal | ACS Medicinal Chemistry Letters |
Volume | 2 |
Issue number | 7 |
DOIs | |
State | Published - Jul 14 2011 |
Externally published | Yes |
Keywords
- Alzheimer's disease
- PET
- fluorine-18
- oxazolo[5,4-b]pyridine
- positron emission tomography
- β-amyloid plaque
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry