Synthesis and structure–activity relationship (SAR) studies of 1,2,3-triazole, amide, and ester-based benzothiazole derivatives as potential molecular probes for tau protein

Author:

Wongso Hendris123ORCID,Ono Maiko4,Yamasaki Tomoteru5,Kumata Katsushi5,Higuchi Makoto4,Zhang Ming-Rong5ORCID,Fulham Michael J.6ORCID,Katsifis Andrew6ORCID,Keller Paul A.1ORCID

Affiliation:

1. School of Chemistry and Molecular Bioscience, Molecular Horizons, University of Wollongong, Wollongong, NSW 2522, Australia

2. Research Center for Radioisotope, Radiopharmaceutical, and Biodosimetry Technology, National Research and Innovation Agency, Puspiptek, Banten 15314, Indonesia

3. Research Collaboration Center for Theranostic Radiopharmaceuticals, National Research and Innovation Agency, Sumedang 45363, Indonesia

4. Department of Functional Brain Imaging, National Institutes for Quantum Science and Technology, Chiba 263-8555, Japan

5. Department of Advanced Nuclear Medicine Sciences, National Institutes for Quantum Science and Technology, Chiba 263-8555, Japan

6. Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW 2050, Australia

Abstract

A series of tau ligands was synthesized replacing the photoisomerisable trans-diene bridge of PBB3 with 1,2,3-triazole, amide, and ester moieties. Several ligands were able to visualise Aβ plaques and neurofibrillary tangles in Alzheimer's disease.

Funder

Kementerian Riset dan Teknologi/Badan Riset dan Inovasi Nasional

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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