178804-18-7Relevant articles and documents
TARGETED ABERRANT ALPHA-SYNUCLEIN SPECIES AND INDUCED UBIQUITINATION AND PROTEOSOMAL CLEARANCE VIA CO-RECRUITMENT OF AN E3-LIGASE SYSTEM
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, (2022/02/06)
Disclosed are bispecific compounds (degraders) that target α-synuclein protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative diseases.
For nerve degenerative disease is in the field of PET imaging agent precursor and the standard method for the synthesis of (by machine translation)
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Paragraph 0074-0076, (2017/01/26)
A novel PET imaging agent precursor and standard and its preparation method, in order to 4-nitro cinnamic aldehyde, the methoxylphenylboronic ethylamine as a reaction initiator, synthesis of the precursor (compound 10) 4 - (6 - (2-P-toluene-sulfonic acid ethoxycarbonyl)-oxy-2-quinolyl)-N-tert-butoxy-carbonyl-N-n-pentyl-( [N-methyl-N-tert-butoxy carbonyl] - 2 - [4 ˊ - (methylamino) phenyl]-benzothiazole aniline) - 6-ether) aniline and standard (compound 25) 4 - (6 - (2-F)-oxy-2-quinolyl)-N-n-pentyl-( [N-methyl] - 2 - [4 ˊ - (methylamino) phenyl]-benzothiazole aniline) - 6-ether) aniline, at the same time provides A β protein specific binding agent 11 C-6-OH-BTA-1 an important intermediate for preparing (compound 7) method for the preparation of, the preparation method is a brand new synthetic route, step is simple, moderate reaction. (by machine translation)
Synthesis and evaluation of two uncharged 99mTc-labeled derivatives of thioflavin-T as potential tracer agents for fibrillar brain amyloid
Serdons,Vanderghinste,Van Eeckhoudt,Cleynhens,De Groot,Bormans,Verbruggen
experimental part, p. 227 - 235 (2010/06/14)
Thioflavin-T is a fluorescent dye for in vitro detection of fibrillar amyloid b, a protein found in the brain of patients suffering from Alzheimer's disease. We synthesized and biologically evaluated two uncharged 99mTc-labeled derivatives of thioflavin-T. The precursors for labeling were synthesized by coupling an S,S′-bis-triphenylmethyl-N-tert- butoxycarbonyl bis-amino-bis-thiol tetradentate ligand via a propoxy spacer to 2-(4′-aminophenyl)-1,3-benzothiazole at the 6-position or the 2′-position. Deprotection and labeling with 99mTc were done via a one-pot procedure (15% yield) after which the labeled compound was isolated by high performance liquid chromatography (LC). LC in combination with mass spectrometry (MS) was used for identity confirmation of the labeled compounds. Results of electrophoresis and log P determination supported the assumption that the radiolabeled compounds could cross the blood-brain barrier by passive diffusion. However, in normal mice both compounds showed a low brain uptake 2 min post injection. They were mainly excreted through the hepatobiliary system, with some accumulation in the stomach. Sixty minutes after intravenous injection, 37% of the 99mTc-activity in the blood corresponded to the original compound. In view of the low brain uptake, it is concluded that the studied 99mTc-labeled derivatives of thioflavin-T are not suitable as tracer agents for in vivo visualization of amyloid in brain. Copyright