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

Yujue Wang, Truc T. Huynh, Nilantha Bandara, Hong Jun Cho, Buck E. Rogers, Liviu M. Mirica

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)1216-1224
Number of pages9
JournalDalton Transactions
Volume51
Issue number3
DOIs
StatePublished - Jan 21 2022

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