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排序方式: 共有912条查询结果,搜索用时 793 毫秒
1.
Optical Review - This paper demonstrates a method to estimate the depth of a fluorescence object in turbid media using dual-wavelength excited photodynamic diagnosis, to aid in the invasion depth... 相似文献
2.
Chris H. Hill Agnete H. Viuff Samantha J. Spratley Stéphane Salamone Stig H. Christensen Randy J. Read Nigel W. Moriarty Henrik H. Jensen Janet E. Deane 《Chemical science》2015,6(5):3075-3086
Krabbe disease is a devastating neurodegenerative disorder characterized by rapid demyelination of nerve fibers. This disease is caused by defects in the lysosomal enzyme β-galactocerebrosidase (GALC), which hydrolyzes the terminal galactose from glycosphingolipids. These lipids are essential components of eukaryotic cell membranes: substrates of GALC include galactocerebroside, the primary lipid component of myelin, and psychosine, a cytotoxic metabolite. Mutations of GALC that cause misfolding of the protein may be responsive to pharmacological chaperone therapy (PCT), whereby small molecules are used to stabilize these mutant proteins, thus correcting trafficking defects and increasing residual catabolic activity in cells. Here we describe a new approach for the synthesis of galacto-configured azasugars and the characterization of their interaction with GALC using biophysical, biochemical and crystallographic methods. We identify that the global stabilization of GALC conferred by azasugar derivatives, measured by fluorescence-based thermal shift assays, is directly related to their binding affinity, measured by enzyme inhibition. X-ray crystal structures of these molecules bound in the GALC active site reveal which residues participate in stabilizing interactions, show how potency is achieved and illustrate the penalties of aza/iminosugar ring distortion. The structure–activity relationships described here identify the key physical properties required of pharmacological chaperones for Krabbe disease and highlight the potential of azasugars as stabilizing agents for future enzyme replacement therapies. This work lays the foundation for new drug-based treatments of Krabbe disease. 相似文献
3.
Polyethylene oxide (PEO) based polymer electrolytes with BaTiO3 as filler and Li(C2F5SO2)2N as salt have been examined in lithium polymer batteries. The aluminum disolution potential in PEO-Li(C2F5SO2)2N was estimated to be 4.1 V vs. Li/Li+ at 80 °C, which was compared to that of 3.8 V vs. Li/Li+ in PEO-Li(CF3SO2)2N. The electrical conductivity of the system was measured as a function of O/Li ratio. The highest conductivity was observed
in O/Li=8. The conductivity was 1.65×10−3 S/cm at 80 °C and 1.5×10−5 S/cm at 25 °C. The interfacial resistance of Li/polymer electrolyte/Li annealed at 80 °C for 15 days was lower than 100 Ωcm2.
Paper presented at the 8th EuroConference on Ionics, Carvoeiro, Algarve, Portugal, Sept. 16 – 22, 2001. 相似文献
4.
5.
Adachi I Aihara H Dijkstra HB Enomoto R Fujii H Fujii K Fujii T Fujimoto J Fujiwara N Hayashii H Higashi S Iida N Imanishi A Ikeda H Ishii T Itoh R Iwasaki H Iwata S Kajikawa R Kamae T Kato S Kawabata S Kichimi H Kishida T Kobayashi M Kuroda S Kusuki N Maruyama A Maruyama K Masuda H Matsuda T Miyamoto A Morimoto T Nakamura K Nitoh O Noguchi S Ochiai F Okuno H Okusawa T Ohshima T Ozaki H Sato T Sai F Shimonaka J Shimozawa K Shirahashi A Sugahara R Sugiyama A Suzuki S Suwada T Takahashi K 《Physical review letters》1988,60(2):97-100
6.
Gregory N. Coppin Andrew Hudson Richard A. Jackson Nigel P.C. Simmons 《Journal of organometallic chemistry》1977,131(3):371-375
The formation of the compound RSnX(acac)2 (acac = 2,4-pentanedionato) by reaction of bis(2,4-pentanedionato)tin(II) on a halide RX with R = CH3, C2H5, C4H9, C6H5, CH2I, (C6H5)3SnCH2, (C2H5)3SnCH2 and X = I, Br has been studied by polarography. At 25°C, it is in fact an equilibrium whose constant has been measured. The intermediate formation of the ion-pair [RSn(acac)2+X?] has allowed us to explain the experimental results. 相似文献
7.
The synthesis of the alkaloid jamtine and the antidepressant paroxetine have been addressed by a strategy involving asymmetric desymmetrisation of prochiral imides by a chiral lithium amide base. A short reaction sequence, starting with a cyclohexane fused succinimide, led to the structures originally reported for the alkaloid jamtine and its derived N-oxide. The structures synthesised are shown not to correspond with those originally reported. A second sequence involves desymmetrisation of a 4-arylglutarimide, and provides a short enantioselective synthesis of the drug substance paroxetine. 相似文献
8.
Peter C. Cherry Derek N. Evans Christopher E. Newall Nigel S. Watson Peter Murray-Rust Judith Murray-Rust 《Tetrahedron letters》1980,21(6):561-564
1,4-Addition of sulphur nucleophiles to the diene () derived the pen-2-em () from clavulanic acid provides the thiadeoxa analogues (–). X-ray analysis of the ester () shows the thermodynamically stable isomers to have the same relative stereochemistry as clavulanic acid. 相似文献
9.
Background
Kynureninase is a key enzyme on the kynurenine pathway of tryptophan metabolism. One of the end products of the pathway is the neurotoxin quinolinic acid which appears to be responsible for neuronal cell death in a number of important neurological diseases. This makes kynureninase a possible therapeutic target for diseases such as Huntington's, Alzheimer's and AIDS related dementia, and the development of potent inhibitors an important research aim. 相似文献10.
Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent
Alkylation of 2-methoxyethoxyphenyl phenyl methane using sec-BuLi and (−)-sparteine has been carried out in excellent yields and up to 94% ee. The best results were obtained in allylation reactions but methylation, ethylation, benzylation and trimethylsilylation have all been carried out with acceptable ee. 相似文献