Literature DB >> 34951428

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

Yujue Wang1, Truc T Huynh2,3, Nilantha Bandara2, Hong-Jun Cho1, Buck E Rogers2, Liviu M Mirica1,4.   

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.

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Year:  2022        PMID： 34951428      PMCID： PMC8969080          DOI： 10.1039/d1dt02767k

Source DB:  PubMed          Journal:  Dalton Trans        ISSN： 1477-9226            Impact factor:   4.390


  45 in total

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  1 in total

1.  68Ga-Labeled Benzothiazole Derivatives for Imaging Aβ Plaques in Cerebral Amyloid Angiopathy.

Authors:  Truc T Huynh; Yujue Wang; Karna Terpstra; Hong-Jun Cho; Liviu M Mirica; Buck E Rogers
Journal:  ACS Omega       Date:  2022-06-06
  1 in total

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