15753-85-2Relevant articles and documents
α-Diketocarboxylic Acids and Their Esters Act as Carbonic Anhydrase IX and XII Selective Inhibitors
Nocentini, Alessio,Lucidi, Alessia,Perut, Francesca,Massa, Annamaria,Tomaselli, Daniela,Gratteri, Paola,Baldini, Nicola,Rotili, Dante,Mai, Antonello,Supuran, Claudiu T.
, p. 661 - 665 (2019)
Among human carbonic anhydrase (CA) inhibitors, the α,I-diketocarboxylic acids and esters are still poorly investigated. Here, we report the first compounds of this class (1-6) acting as potent inhibitors at low nanomolar level against the cancer-related
Dioxolone structure containing 4 - N substituted quinazoline derivatives and its preparation and use (by machine translation)
-
, (2017/11/16)
The invention discloses a dioxolone structure containing 4 -NSubstituted quinazoline derivatives, its structure such as shown in I. This invention has introduced to substituted benzoic acid, methanol, nitric acid, formamide, trichloro oxygen phosphorus chlorine, nitrobenzene formaldehyde, acetone, stannous chloride, substituted aromatic aldehyde as raw material, by the multi-step reaction to synthesize the target compound. The compounds can be used as anti-tumor, anti-bacterial plant and anti-plant-virus of the drug. (1 E, 4 E) - 1 - substituted phenyl - 5 - (4 - (substituted quinazoline - 4 - amino) phenyl) - 1, 4 - pentadiene - 3 - one. (by machine translation)
Palladium nanoparticles supported on copper oxide as an efficient and recyclable catalyst for carbon(sp2)-carbon(sp2) cross-coupling reaction
Nasrollahzadeh, Mahmoud,Sajadi, S. Mohammad,Rostami-Vartooni, Akbar,Azarian, Abbas
, p. 150 - 154 (2015/04/14)
A convenient, mild and cost-effective synthesis of Pd/CuO nanoparticles by arc discharge of Cu in deionized (DI) water and electroless deposition of palladium was reported. The obtained nanoparticles were thoroughly characterized by using techniques like TEM, XRD, FE-SEM and EDS. The synthesized nanoparticles demonstrated excellent catalytic activity in Heck coupling reaction under aerobic conditions. The effects of catalyst composition, solvent and bases, aryl halides or olefins species on corresponding products were systematically investigated. High product yields, elimination of ligand and homogeneous catalysts, broad substrate scope and easy work up are important features of this method. In addition, the catalyst could be reused for five more consecutive recycles.
Novel 18F-labeled dibenzylideneacetone derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques
Li, Zijing,Cui, Mengchao,Zhang, Jinming,Dai, Jiapei,Zhang, Xiaojun,Chen, Peng,Jia, Hongmei,Liu, Boli
, p. 628 - 638 (2014/08/18)
A series of dibenzylideneacetones were synthesized and evaluated as imaging probes for β-amyloid plaques. They displayed high binding affinity to Aβ1-42 aggregates (Ki = 6.4 for 8, Ki = 3.0 for 9), and the high binding wer
Preparation of monometallic (Pd, Ag) and bimetallic (Pd/Ag, Pd/Ni, Pd/Cu) nanoparticles via reversed micelles and their use in the Heck reaction
Heshmatpour, Felora,Abazari, Reza,Balalaie, Saeed
experimental part, p. 3001 - 3011 (2012/05/31)
The metal nanoparticles (NPs) have been prepared using a water-in-oil microemulsion system of water/dioctyl sulfosuccinate sodium salt (aerosol-OT, AOT)/isooctane at 25 °C. Since the NPs produced in this system can endure forcing conditions (100 °C), this system has been used for the synthesis of nano-catalysts in the Heck reactions. FE-SEM, DLS, and UV/vis analyses have been used to characterize the surface morphology, size, and proof of the formation of all the prepared metal NPs, respectively. In addition, the effects of some reaction parameters (here, bases and solvents) were optimized. Differences in the catalytic properties of the synthesized NPs have also been investigated. Consequently, the Pd/Cu (4:1) bimetallic NP showed the highest activity in the C-C coupling reaction of the iodobenzene with the styrene, thus it is employed as the superior catalyst in this study. Therefore, the Pd/Cu (4:1) bimetallic NPs were further investigated using TEM and XRD analyses. This catalyst system is also reusable for six runs with very negligible reduction in the efficiency.
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.
Room temperature aldol reactions using magnetic Fe3O 4@Fe(OH)3 composite microspheres in hydrogen bond catalysis
Niu, Fang,Zhang, Long,Luo, San-Zhong,Song, Wei-Guo
supporting information; scheme or table, p. 1109 - 1111 (2010/06/18)
Fe3O4@Fe(OH)3 composite microspheres are highly active, environmentally friendly and easy to recycle catalysts for aldol reactions, which are catalyzed by a solid-liquid interfacial hydrogen bond catalyst at room temperature.