Issue 3, 2022

2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for 64Cu PET imaging in Alzheimer's disease

Abstract

Herein we report a new series of bifunctional chelators (BFCs) with high affinity for amyloid β aggregates, strong binding affinity towards Cu(II), and favorable lipophilicity for potential blood–brain barrier (BBB) penetration. The alkyl carboxylate ester pendant arms show high binding affinity towards Cu(II). The BFCs form stable 64Cu-radiolabeled complexes and exhibit favorable partition coefficient (log D) values of 0.75–0.95. Among the five compounds tested, 64Cu-YW-1 and 64Cu-YW-13 complexes exhibit significant staining of amyloid plaques in ex vivo autoradiography studies.

Graphical abstract: 2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for 64Cu PET imaging in Alzheimer's disease

Supplementary files

Article information

Article type
Paper
Submitted
18 Aug 2021
Accepted
10 Dec 2021
First published
15 Dec 2021

Dalton Trans., 2022,51, 1216-1224

2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for 64Cu PET imaging in Alzheimer's disease

Y. Wang, T. T. Huynh, N. Bandara, H. Cho, B. E. Rogers and L. M. Mirica, Dalton Trans., 2022, 51, 1216 DOI: 10.1039/D1DT02767K

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