1285534-59-9Relevant academic research and scientific papers
Radiosynthesis and preliminary biological evaluation of a new 18F-labeled triethylene glycol derivative of triphenylphosphonium
Tominaga, Takahiro,Ito, Hiroaki,Ishikawa, Yoichi,Iwata, Ren,Ishiwata, Kiichi,Furumoto, Shozo
, p. 117 - 123 (2016/03/12)
Delocalized lipophilic cations such as [18F]fluorobenzyltriphenylphosphonium ([18F]FBnTP) can accumulate in mitochondria and have been used in myocardial perfusion imaging (MPI). In this study, we established a simplified method for
Radiolabeled pyridinyl analogues of dibenzylideneacetone as β-amyloid imaging probes
Cui, Xiaomei,Zhang, Xiaoyang,Peng, Cheng,Dai, Jiapei,Liu, Boli,Cui, Mengchao
, p. 44646 - 44654 (2016/06/09)
In continuation of our investigation of the dibenzylideneacetone scaffold as Aβ imaging probes, a series of derivatives containing pyridine rings with lower lipophilicity was synthesized and evaluated. Some of these probes displayed high affinities to Aβ
Reductive carbonylation of aryl halides employing a two-chamber reactor: A protocol for the synthesis of aryl aldehydes including 13C- and D-isotope labeling
Korsager, Signe,Taaning, Rolf H.,Lindhardt, Anders T.,Skrydstrup, Troels
, p. 6112 - 6120 (2013/07/26)
A protocol has been developed for conducting the palladium-catalyzed reductive carbonylation of aryl iodides and bromides using 9-methylfluorene-9- carbonyl chloride (COgen) as a source of externally delivered carbon monoxide in a sealed two-chamber system (COware), and potassium formate as the in situ hydride source. The method is tolerant to a wide number of functional groups positioned on the aromatic ring, and it can be exploited for the isotope labeling of the aldehyde group. Hence, reductive carbonylations run with 13COgen provide a facile access to 13C-labeled aromatic aldehydes, whereas with DCO2K, the aldehyde is specifically labeled with deuterium. Two examples of double isotopic labeling are also demonstrated. Finally, the method was applied to the specific carbon-13 labeling of the β-amyloid binding compound, florbetaben.
Synthesis and structure-affinity relationships of novel dibenzylideneacetone derivatives as probes for ?-Amyloid Plaques
Cui, Mengchao,Ono, Masahiro,Kimura, Hiroyuki,Liu, Boli,Saji, Hideo
experimental part, p. 2225 - 2240 (2011/06/17)
A new and extensive set of dibenzylideneacetone derivatives was synthesized and screened for affinity toward A1-42 aggregates. Structure-activity relationships revealed the binding of dibenzylideneacetones to be affected by various substituents. The introduction of a substituent group in the ortho position reduced or abolished the binding. However, the para position was highly tolerant of sterically demanding substitutions. Three radioiodinated ligands (6, 70, and 71) and two 18F fluoro-pegylated (FPEG) ligands (83 and 85) were prepared, all of which displayed high affinity for A1-42 aggregates (Ki ranging from 0.9 to 7.0 nM). In biodistribution experiments, they exhibited good initial penetration (1.59, 4.68, 4.56, 4.13, and 5.15% ID/g, respectively, at 2 min) of and fast clearance from the brain. Autoradiography with sections of postmortem AD brain and transgenic mouse brain confirmed the high affinity of these tracers. These preliminary results strongly suggest the dibenzylideneacetone structure to be a potential new scaffold for β-amyloid imaging probes.
