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Aromatic radiofluorination and biological evaluation of 2-aryl-6-[ 18F]fluorobenzothiazoles as a potential positron emission tomography imaging probe for β-amyloid plaques

Title
Aromatic radiofluorination and biological evaluation of 2-aryl-6-[ 18F]fluorobenzothiazoles as a potential positron emission tomography imaging probe for β-amyloid plaques
Authors
Lee B.C.Kim J.S.Kim B.S.Son J.Y.Hong S.K.Park H.S.Moon B.S.Jung J.H.Jeong J.M.Kim S.E.
Ewha Authors
김범산
SCOPUS Author ID
김범산scopus
Issue Date
2011
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 19, no. 9, pp. 2980 - 2990
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
To develop agents for radionuclide imaging Aβ plaques in vivo, we prepared three fluorine-substituted analogs of arylbenzothiazole class; compound 2 has a high affinity for Aβ (Ki = 5.5 nM) and the specific binding to Aβ in fluorescent staining. In preparation for the synthesis of these arylbenzothiazole analogs in radiolabeled form as an Aβ plaques-specific positron emission tomography (PET) imaging probe, we investigated synthetic route suitable for its labeling with the short-lived PET radionuclide fluorine-18 (t1/2 = 110 min) and diaryliodonium tosylate precursors (12, 13a-e and 14). 2-Aryl-6-[18F]fluorobenzothiazoles ([18F]1-3) were synthesized in efficiently short reaction times (40-60 min) with high radiochemical yields (19-40%), purities (>95%) and specific activities (85-118 GBq/μmol). Tissue distribution studies showed that high radioactivity of [18F]2 accumulated in the brain with rapid clearance in healthy mice. Radioactive metabolites were analyzed in brain samples of mice and corresponded to 81% of parent remained by 30 min after a tail-vein injection. These results suggest that [18F]2 is a promising probe for evaluation of Aβ plaques imaging in brain using PET. © 2011 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2011.03.029
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의학전문대학원 > 의학과 > Journal papers
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