Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Victoria 3086, Australia.
School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Parkville, Victoria 3010, Australia.
Dalton Trans. 2020 Apr 7;49(14):4559-4569. doi: 10.1039/c9dt04687a.
Two tridentate ligand systems bearing N-heterocyclic carbene (NHC), amine and carboxylate donor groups coupled to benzothiazole- or stilbene-based amyloid binding moieties were synthesised. Reaction of the imidazolium salt containing pro-ligands with Re(CO)5Cl yielded the corresponding rhenium metal complexes which were characterised by NMR, and X-ray crystallography. These ligands are of interest for the potential preparation of technetium-99m imaging agents for Alzheimer's disease and the capacity of these rhenium complexes bind to amyloid fibrils composed of amyloid-β peptide and amyloid plaques in human frontal cortex brain tissue was evaluated using fluorescence microscopy. These studies show that the complexes bound efficiently to amyloid-β fibrils and some evidence of binding to amyloid-β plaques.
合成了两种含有氮杂环卡宾（NHC）、胺和羧酸盐供体基团的三齿配体系统，这些配体与苯并噻唑或二苯乙烯基淀粉样蛋白结合部分偶联。用含有前配体的咪唑鎓盐与 Re(CO)5Cl 反应，得到相应的铼金属配合物，通过 NMR 和 X 射线晶体学进行了表征。这些配体对于潜在的制备用于阿尔茨海默病的锝-99m 成像剂具有重要意义，并且评估了这些铼配合物与由人额皮质脑组织中的淀粉样β肽和淀粉样斑块组成的淀粉样纤维结合的能力，使用荧光显微镜。这些研究表明，这些配合物有效地与淀粉样β纤维结合，并证明与淀粉样β斑块有一定的结合。
