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

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 tow...

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Published inDalton transactions : an international journal of inorganic chemistry Vol. 51; no. 3; pp. 1216 - 1224
Main Authors Wang, Yujue, Huynh, Truc T, Bandara, Nilantha, Hong-Jun, Cho, Rogers, Buck E, Mirica, Liviu M
Format Journal Article
LanguageEnglish
Published Cambridge Royal Society of Chemistry 17.01.2022
Subjects
Affinity
Alzheimer's disease
Autoradiography
Binding
Blood-brain barrier
Chelating agents
Positron emission
Tomography
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Summary: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.
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ISSN:1477-9226
1477-9234
DOI:10.1039/d1dt02767k