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301.
Nishida H Mukaihira T Saitoh F Harada K Fukui M Matsusue T Okamoto A Hosaka Y Matsumoto M Shiromizu I Ohnishi S Mochizuki H 《Chemical & pharmaceutical bulletin》2004,52(4):406-412
In the course of development of factor Xa (FXa) inhibitor in an investigation involving the synthesis of 1-arylsulfonyl-3-piperazinone derivatives, we found new compounds containing a unique spiro skeleton. Among such compounds, (-)-7-[(6-chloro-2-naphthalenyl)sulfonyl]tetrahydro-8a-(methoxymethyl)-1'-(4-pyridinyl)-spiro[5H-oxazolo[3,2-a]pyrazine-2(3H),4'-piperidin]-5-one (28, M55529) had activity more favorable than those of previously reported compounds. The inhibitory activity of M55529 for FXa is IC(50)=2 nM, with high selectivity for FXa over thrombin and trypsin. 相似文献
302.
A stable Ru(II)/Ru(III) mixed-valence state was observed in acetonitrile for the ruthenium binuclear complex bridged by dimercaptothiadiazolate (DeltaE(1/2) = 220 mV for Ru(2)(II,II)/Ru(2)(II,III) and Ru(2)(II,III)/Ru(2)(III,III) processes; K(com) = 5.3 x 10(3)). Upon protonation of the bridging ligand by the addition of equimolar p-toluenesulfonic acid, however, the mixed-valence state diminished (DeltaE(1/2) = 0 mV). The bridging ligand operates as a proton-induced switch of the electronic communication in the dimeric complex. 相似文献
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The combined use of chiral Pd complex 2 and amine salt enabled completely regulated release of free nucleophilic amine. Under these conditions, an efficient catalytic asymmetric conjugate addition of various amines was achieved to afford beta-amino acid derivatives in high chemical yields with up to 98% ee. Furthermore, a highly enantioselective protonation in 1,4-addition of amine was also developed. [reaction: see text] 相似文献
306.
Novel molecular recognition via fluorescent resonance energy transfer using a biotin-PEG/polyamine stabilized CdS quantum dot 总被引:2,自引:0,他引:2
Nagasaki Y Ishii T Sunaga Y Watanabe Y Otsuka H Kataoka K 《Langmuir : the ACS journal of surfaces and colloids》2004,20(15):6396-6400
A novel functionally PEGylated quantum dot (QD) was prepared by a coprecipitation method in the presence of the biotin-PEG/polyamine block copolymer. When CdCl2 and Na2S were mixed in aqueous media in the presence of the biotin-PEG-b-poly(2-(N,N-dimethylamino)ethyl methacrylate) [biotin-PEG/PAMA], a CdS QD with a size of ca. 5 nm was prepared. The polyamine segment was anchored on the surface of the formed CdS nanoparticle, whereas the PEG segment was tethered on the surface to form a hydrophilic palisade, thus improving the dispersion stability in aqueous media even under a high salt concentration condition. An effective fluorescent resonance energy transfer (FRET) was observed by the specific interaction of the biotin-PEG/PAMA stabilized CdS QD with TexasRed-labeled streptavidin of the physiological ionic strength of 0.15 M. The extent of the energy transfer was in proportion to the concentration of the TexasRed-streptavidin. This FRET system using the PEGylated CdS QD coupled with fluorescent-labeled protein can be utilized as a highly sensitive bioanalytical system. 相似文献
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In the selection of an appropriate material which satisifes the impact strength requirement for an injection moduled product, the Charpy, Izod or dart drop test methods should be used according to the impact mode displayed by the product—that is, either snap impact on a bar or impact on a shell structure—because generally the ranking of a material determined by the Charpy test differs from that determined by the dart drop test. However, preference for the Charpy test, because of the advantage of simples evaluation work, sometimes leads to erroneous judgement of product characteristics. The breaking behaviour of various materials as determined by Charpy apparatus equipped with instrumentation was studied, and a new design of Charpy test was shown to correlate with the dart drop impact test. The procedure used was to provide a bigger notch tip radius, to break the specimen parallel to the flow direction in the injection moulding process, and to apply the energy absorbed until the beginning of fracture at the notch end. 相似文献
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Aihara H Jaquinod L Nurco DJ Smith KM 《Angewandte Chemie (International ed. in English)》2001,40(18):3439-3441