83073-86-3Relevant academic research and scientific papers
Beta-amyloid protein targeting fluorescent probe, preparation and application of beta-amyloid protein targeting fluorescent probe in Alzheimer's disease
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Paragraph 109; 0229-0233, (2021/06/09)
The invention discloses a beta-amyloid protein targeting fluorescent probe, preparation and application of the beta-amyloid protein targeting fluorescent probe in Alzheimer's disease. The structural formula of the fluorescent probe is as shown in formula I in the specification. The fluorescent probe disclosed by the invention is a compound taking 6-dimethylamino-1-methylquinoline as a parent structure, and the fluorescent probe has the advantages of long emission wavelength, large Stock shift, capability of specifically detecting beta amyloid protein, sensitivity to viscosity in tissue cells, and good response to the viscosity. After the fluorescent probe is combined with beta amyloid protein in the brain of a patient suffering from the Alzheimer's disease, a fluorescence signal is obviously enhanced, and the fluorescent probe can be used for detecting the beta amyloid protein and early diagnosing the Alzheimer's disease and has important guiding significance on development of diagnosis and treatment probes of the Alzheimer's disease.
With the plaque and A β of the nerve fiber entanglement having affinity to the compound and its preparation method
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Paragraph 0129-0130, (2018/04/26)
The invention provides a compound provided with good affinity and tangled with an Abeta plaque and a nerve fiber. The structural general formula (I) of the compound is as shown in the specification, wherein W is a benzo-hexahydric aromatic ring or a hexah
A Difluoroboron β-Diketonate Probe Shows turn-on Near-Infrared Fluorescence Specific for Tau Fibrils
Park, Kwang-Su,Kim, Mi Kyoung,Seo, Yujin,Ha, Taewoong,Yoo, Kyeongha,Hyeon, Seung Jae,Hwang, Yu Jin,Lee, Junghee,Ryu, Hoon,Choo, Hyunah,Chong, Youhoon
, p. 2124 - 2131 (2017/10/23)
Tau aggregation in neuronal cells has recently received significant attention as a robust predictor of the progression of Alzheimer's disease (AD) because of its proven correlation with the degree of cognitive impairment in AD patients. Accordingly, noninvasive imaging of tau aggregates has been highlighted as a promising diagnostic tool for AD. We have previously identified a tau-specific turn-on near-infrared fluorescent (NIRF) probe (1), and, in this study, structural modification was performed to optimize its physicochemical as well as fluorescence properties. Thus, a series of fluorescent dyes (2a-2j) composed of a variously substituted difluoroboron β-diketonate and an N,N-dimethylaniline moiety linked by a length-extendable π-bridge were prepared. Among those, isobutyl-substituted difluoroboron β-ketonate with a π-conjugated 1,4-butadienyl linker (2e) showed the most promising properties as a tau-specific NIRF probe. Compared with 1, the turn-on fluorescence of 2e was more specific to tau fibrils, and it showed 8.8- and 6.2-times higher tau-over-Aβ and tau-over-BSA specificity, respectively. Also, the fluorescence intensity of 2e upon binding to tau fibrils was substantially higher (~2.9 times) than that observed from 1. The mechanism for tau-specificity of 2e was investigated, which suggested that the molecular rotor-like property of 2e enables specific recognition of the microenvironment of tau aggregates to emit strong fluorescence. In transgenic cell lines stably expressing GFP-tagged tau proteins, 2e showed good colocalization with tau-GFP. Moreover, the fluorescence from 2e exhibited almost complete overlap with p-Tau antibody staining in the human AD brain tissue section. Collectively, these observations demonstrate the potential of 2e as a tau-specific fluorescent dye in both in vitro and ex vivo settings.
Structure-activity relationships of radioiodinated diphenyl derivatives with different conjugated double bonds as ligands for α-synuclein aggregates
Ono, Masahiro,Doi, Yuki,Watanabe, Hiroyuki,Ihara, Masafumi,Ozaki, Akihiko,Saji, Hideo
, p. 44305 - 44312 (2016/06/09)
It is generally recognized that aggregates of α-synuclein (α-syn) in the brain are closely associated with the pathogenesis of Parkinson's disease (PD). Therefore, the development of in vivo imaging probes targeting α-syn aggregates is currently expected.
A convenient synthetic entry into aldehydes with extended conjugation
Friedli, Andrienne C.,Yang, Edward,Marder, Seth R.
, p. 2717 - 2730 (2007/10/03)
Variable-length donor-acceptor polyenes 1-18 were synthesized. In the key step, a polyenal was appended to an aromatic donor through nucleophilic attack of an organolithium reagent on a vinylogous amide. Yields of aldehydes and dialdehydes in the one-pot process ranged from 12-64% and depended upon number of repeat units (n=1-3) in the polyene chain.
