Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 10, Pages 2966-2968Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.052
Keywords
2-Aryl-imidazo[2,1-b]benzothiazole; beta-Amyloid; Alzheimer's disease; PET imaging; SPECT imaging
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We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (K-i = 6 nM) can be labeled with (CH3)-C-11 for PET imaging whereas 3j (K-i = 10.9 nM) can be labeled with I-123 for SPECT imaging. (C) 2011 Elsevier Ltd. All rights reserved.
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