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.
| Autor: | Wongso H; School of Chemistry and Molecular Bioscience, Molecular Horizons, University of Wollongong Wollongong NSW 2522 Australia keller@uow.edu.au.; Research Center for Radioisotope, Radiopharmaceutical, and Biodosimetry Technology, National Research and Innovation Agency Puspiptek Banten 15314 Indonesia.; Research Collaboration Center for Theranostic Radiopharmaceuticals, National Research and Innovation Agency Sumedang 45363 Indonesia., Ono M; Department of Functional Brain Imaging, National Institutes for Quantum Science and Technology Chiba 263-8555 Japan., Yamasaki T; Department of Advanced Nuclear Medicine Sciences, National Institutes for Quantum Science and Technology Chiba 263-8555 Japan., Kumata K; Department of Advanced Nuclear Medicine Sciences, National Institutes for Quantum Science and Technology Chiba 263-8555 Japan., Higuchi M; Department of Functional Brain Imaging, National Institutes for Quantum Science and Technology Chiba 263-8555 Japan., Zhang MR; Department of Advanced Nuclear Medicine Sciences, National Institutes for Quantum Science and Technology Chiba 263-8555 Japan., Fulham MJ; Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital Camperdown NSW 2050 Australia., Katsifis A; Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital Camperdown NSW 2050 Australia., Keller PA; School of Chemistry and Molecular Bioscience, Molecular Horizons, University of Wollongong Wollongong NSW 2522 Australia keller@uow.edu.au. |
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| Jazyk: | angličtina |
| Zdroj: | RSC medicinal chemistry [RSC Med Chem] 2023 Jan 27; Vol. 14 (5), pp. 858-868. Date of Electronic Publication: 2023 Jan 27 (Print Publication: 2023). |
| DOI: | 10.1039/d2md00358a |
| Abstrakt: | The pyridinyl-butadienyl-benzothiazole (PBB3 15) scaffold was used to develop tau ligands with improved in vitro and in vivo properties for imaging applications to provide insights into the etiology and characteristics of Alzheimer's disease. The photoisomerisable trans -butadiene bridge of PBB3 was replaced with 1,2,3-triazole, amide, and ester moieties and in vitro fluorescence staining studies revealed that triazole derivatives showed good visualisation of Aβ plaques, but failed to detect the neurofibrillary tangles (NFTs) in human brain sections. However, NFTs could be observed using the amide 110 and ester 129. Furthermore, the ligands showed low to high affinities ( K Competing Interests: There are no conflicts to declare. (This journal is © The Royal Society of Chemistry.) |
| Databáze: | MEDLINE |
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