biostudies-literatureWang YNIGMS NIH HHS1216-1224https://www.ebi.ac.uk/biostudies/studies/S-EPMC8969080biostudies-literatureUnknown51(3)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 <i>D</i>) 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 <i>ex vivo</i> autoradiography studies.Dalton transactions (Cambridge, England : 2003)2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for ⁶⁴Cu PET imaging in Alzheimer's disease.PMC8969080R01 GM114588Rogers BEMirica LMCho HJWang YBandara NHuynh TTfalse2-(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 towards Cu(II). The BFCs form stable ⁶⁴Cu-radiolabeled complexes and exhibit favorable partition coefficient (log <i>D</i>) 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 <i>ex vivo</i> autoradiography studies.2022-01-01T00:00:00Z2022 Jan2025-04-19T12:43:37.163Z2025-04-19T12:43:37.163ZS-EPMC89690803495142810.1039/d1dt02767k