111934-94-2Relevant articles and documents
CRYSTAL OF CYCLIC PHOSPHONIC ACID SODIUM SALT AND METHOD FOR MANUFACTURING SAME
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Paragraph 0362; 0363, (2017/09/02)
An object of the present invention is to provide a crystal of a cyclic phosphonic acid sodium salt (2ccPA) with high purity and excellent storage stability and a method for producing the crystal. The present invention provides a crystal of a cyclic phosphonic acid sodium salt (2ccPA) represented by formula (1):
F-18 stilbenes as PET imaging agents for detecting β-amyloid plaques in the brain
Zhang, Wei,Oya, Shunichi,Kung, Mei-Ping,Hou, Catherine,Maier, Donna L.,Kung, Hank F.
, p. 5980 - 5988 (2007/10/03)
Imaging agents targeting β-amyloid (Aβ) may be useful for diagnosis and treatment of patients with Alzheimer's disease (AD). Compounds 3e and 4e are fluorinated stilbene derivatives displaying high binding affinities for Aβ plaques in AD brain homogenates (Ki = 15 ± 6 and 5.0 ± 1.2 nM, respectively). In vivo biodistributions of [ 18F]Se and [18F]4e in normal mice exhibited excellent brain penetrations (5.55 and 9.75% dose/g at 2 min), and rapid brain washouts were observed, especially for [18F]4e (0.72% dose/g at 60 min). They also showed in vivo plaque labeling in APP/PS1 or Tg2576 transgenic mice, animal models for AD. Autoradiography of postmortem AD brain sections and AD homogenate binding studies confirmed the selective and specific binding properties to Aβ plaques. In conclusion, the preliminary results strongly suggest that these fluorinated stilbene derivatives, [18F]3e and [18F]4e, are suitable candidates as Aβ plaque imaging agents for studying patients with AD.
Synthesis and Evaluation of Phospholipid Analogues as Inhibitors of Cobra Venom Phospholipase A2
Yuan, Wei,Berman, Richard J.,Gelb, Michael H.
, p. 8071 - 8081 (2007/10/02)
Analogues of phospholipids that contain fluoro ketone, ketone, and alcohol replacements for the ester at the 2-position of the glycerol backbone have been prepared and analyzed as inhibitors of phospholipase A2 from Naja naja naja venom.Phospholipid analogues were studied that contain two alkyl chains as well as single chain compounds that lack carbon-1 of the glycerol backbone and the attached acyl unit.Compounds that contain both long and medium length alkyl chains were studied.All of the potential inhibitors were tested in a well-defined mixed micelle system in which both the substrates and the inhibitors have been incorporated into Triton X-100 micelles.Surprisingly, the best inhibitors studied were the single chain fluoro ketones despite the fact that the enzyme has a strong preference for two-chain lipids.The most potent compound was found to have a dissociation constant some 600-3000-fold lower than the Michaelis constant for dipalmitoyl phosphatidylcholine substrate. 19F NMR studies of the fluoro ketone phospholipid analogues in micelles show that whereas the single chain compounds are partially in the hydrated-ketone form, the two-chain compounds are less than 0.1percent hydrated.In every case studied, potent inhibition of phospholipase A2 was observed only with those compounds that are significantly hydrated in the micelle, and it is suggested that the hydrated fluoro ketone containing phospholipid analogues are the species responsible for the inhibition.In addition, the single chain fluoro ketones were better inhibitors than single and double chain alcohol and ketone analogues.Previous studies have been show that the cobra venom enzyme is activated by choline-containing lipids, and evidence is presented for the binding of the hydrated fluoro ketone inhibitors selectively to the activated enzyme.
