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Charge neutral rhenium tricarbonyl complexes of tridentate N-heterocyclic carbene ligands that bind to amyloid plaques of Alzheimer's disease
Dalton Transactions ( IF 4 ) Pub Date : 2020/03/10 , DOI: 10.1039/c9dt04687a
Nuchareenat Wiratpruk 1, 2, 3, 4 , Asif Noor 4, 5, 6, 7 , Catriona A. McLean 4, 6, 7, 8 , Paul S. Donnelly 4, 5, 6, 7 , Peter J. Barnard 1, 2, 3, 4
Affiliation  

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.

中文翻译:

带电荷的中性三齿N-杂环卡宾配体的中性三羰基配合物,可与阿尔茨海默氏病的淀粉样斑块结合

合成了两个带有N-杂环卡宾(NHC),胺和羧酸酯供体基团的三齿配体系统,这些基团与基于苯并噻唑或的淀粉样蛋白结合部分偶联。含原配体的咪唑鎓盐与Re(CO)5 Cl的反应产生相应的rh金属配合物,其通过NMR和X射线晶体学表征。这些配体对于潜在制备用于阿尔茨海默氏病的tech 99m成像剂具有重要意义,并且使用荧光显微镜评估了这些rh络合物与人额叶皮质脑组织中由淀粉样β-肽和淀粉样斑块组成的淀粉样原纤维结合的能力。这些研究表明,该复合物与淀粉样蛋白β原纤维有效结合,并且有与淀粉样蛋白β斑块结合的证据。
更新日期:2020-04-08
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