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Benzothiazole Carboxylate Diester Bifunctional Chelators for 64Cu PET Imaging in Alzheimer’s Disease

preprint
submitted on 07.05.2021, 04:53 and posted on 11.05.2021, 04:30 by Yujue Wang, Truc T. Huynh, Nilantha Bandara, Hong-Jun Cho, Buck E. Rogers, Liviu M. Mirica
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 enable 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, the 64Cu-YW-1 and 64Cu-YW-13 complexes exhibit significant staining of amyloid plaques in ex vivo autoradiography studies.

Funding

NIH R01GM114588

History

Email Address of Submitting Author

mirica@illinois.edu

Institution

University of Illinois at Urbana-Champaign

Country

United States

ORCID For Submitting Author

0000-0003-0584-9508

Declaration of Conflict of Interest

no conflict of interest

Version Notes

version 1.0