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151.
A highly oriented structure for Bi2Sr2Ca2Cu3O8 bulk superconductors was successfully made by hot-forging. The Jc values were closely related to the degree of orientation. Microstructure observations and magnetization measurements revealed that the properties of the highly oriented BSCCO reflected the two-dimensionality in this layered structure material. 相似文献
152.
Inoue S Kaji N Kataoka M Shinohara Y Okamoto Y Tokeshi M Baba Y 《Electrophoresis》2011,32(22):3241-3247
We have developed a separation technique for DNA-protein complex based on electrophoretic mobility shift assay (EMSA) by microchip electrophoresis, which we call microchip electrophoretic mobility shift assay (μEMSA). To evaluate the μEMSA, we employed recombinant human nuclear factor-κB (rhNF-κB) and its consensus double-stranded oligonucleotide (dsOligo) fluorescently labeled with Cy5. We carried out the electrophoretic separation of the consensus dsOligo-rhNF-κB complex and the unbound dsOligo in methylcellulose solution and confirmed rapid (~200 s) and reliable identification and semi-quantitation of the specific interaction between dsOligo and rhNF-κB. The binding specificity of rhNF-κB was confirmed by introducing non-fluorescently labeled consensus oligonucleotide as a competitor. The progression of the binding reaction under various incubation times was monitored, and it was found that the dsOligo and rhNF-κB complex formation reached equilibrium (ca. 90% of the dsOligo was bound to rhNF-κB) after 5 min. Furthermore, without any purification process, even crude NF-κB in nuclear extracts from HeLa cells was specifically detected within 120 s by the μEMSA. 相似文献
153.
Yamada Y Hidefumi K Shion H Oshikata M Haramaki Y 《Rapid communications in mass spectrometry : RCM》2011,25(11):1600-1608
In pharmacology and toxicology, localization of the distribution of a drug molecule in its target tissue provides very important in vivo biological information. Traditionally, this has been examined using autoradiography (ARG). However, there are significant limitations in this application. One is the synthesis and use of radiolabeled compounds, the other is that the image generated expresses an undifferentiated mixture of the parent drug and/or its metabolites. The objective of the study was to define the specific distribution of the parent drug in rat ocular tissue containing melanin (e.g. the retina) using non‐labeled chloroquine by MALDI Imaging tandem mass spectrometry (MS/MS). After single oral administration (at 20 mg/kg) of chloroquine, sections (10 µm) of rat eye tissue were prepared at 24 h. The MS system used was a quadrupole time‐of flight (Q‐TOF) tandem mass spectrometer (MALDI Synapt?, Waters, Milford, MA, USA). Tissue sections were sprayed with CHCA (α‐cyano‐4‐hydroxycinnamic acid, 5 mg/mL) in 80% acetonitrile (ACN) containing 5% formic acid (FA) using either a manual sprayer (airbrush) or an automated sprayer (TM‐Sprayer?, HTX Technologies, Carrboro, NC, USA). Chloroquine was readily detected in the MS/MS mode by monitoring one of its major fragment ions (m/z 247.10) and imaged through the rat eye tissue. The image of the specific distribution within the retina in the rat eye tissue was confirmed, and found to be similar to autoradiograms after oral administration of 14C‐chloroquine reported previously. Copyright © 2011 John Wiley & Sons, Ltd. 相似文献
154.
Quinolone Analogues 15: Synthesis and Antimalarial Activity of 4‐Phenyl‐1‐(1‐triazolylmethyl‐4‐quinolon‐3‐ylcarbonyl)semicarbazide and Related Compounds
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Yoshihisa Kurasawa Kiminari Yoshida Naoki Yamazaki Kenji Sasaki Yoshito Zamami Zhao Min Atsumi Togi Hideyuki Ito Eisuke Kaji Haruhiko Fukaya 《Journal of heterocyclic chemistry》2014,51(Z1):E249-E254
The 1‐hydrazinocarbonylmethyl‐4‐quinolone‐3‐carboxylate ( 10 ) was converted into the 1‐(4‐amino‐1,2,4‐triazol‐3‐ylmethyl)‐4‐quinolone‐3‐carboxylic acid ( 13 ), whose reaction with arylcarbaldehydes gave the 1‐(4‐arylmethyleneamino‐1,2,4‐triazol‐3‐ylmethyl)‐4‐quinolone‐3‐carboxylic acids ( 5a , 5b , 5c , 5d , 5e , 5f , 5g ). Compound 10 was also transformed into the 1‐(4‐amino‐1,2,4‐triazol‐3‐ylmethyl)‐4‐quinolone‐3‐carbohydrazide ( 15 ), whose reaction with phenyl isocyanate or phenyl isothiocyanate afforded the 4‐phenyl‐1‐(1‐triazolylmethyl‐4‐quinolon‐3‐ylcarbonyl)semicarbazide ( 6a ) or 4‐phenyl‐1‐(1‐triazolylmethyl‐4‐quinolon‐3‐ylcarbonyl)thiosemicarbazide ( 6b ), respectively. Compounds 6a , 6b showed the in vitro antimalarial activity to chloroquine‐resistant Plasmodium falciparum, wherein their IC50 was 3.89 and 3.91 μM, respectively. 相似文献
155.
Quinolone Analogs 16: A Facile D–H Exchange for 3‐H Proton of 2‐Substituted 4‐Quinolones in Acidic Media
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Yoshihisa Kurasawa Kiminari Yoshida Naoki Yamazaki Kenji Sasaki Yoshito Zamami Zhao Min Atsumi Togi Hideyuki Ito Eisuke Kaji Haruhiko Fukaya 《Journal of heterocyclic chemistry》2014,51(6):1821-1829
The 4‐quinolones having the urea or carbamate moiety at the 2‐position showed the facile deuterium–hydrogen (D–H) exchange of the 3‐H proton in deuteriotrifluoroacetic acid‐deuteriodimethyl sulfoxide (3:1) at 60°C, whereas the 4‐quinolones possessing the carboxylate or carbohydrazide group at the 2‐position and 2‐substituted 4‐methoxyquinolines represented no D –H exchange of the 3‐H proton under the same condition. The aforementioned D–H exchange was found to require both the tautomerization of the 4‐quinolone into 4‐hydroxyquinoline in strongly acidic media and the nitrogen functional group at the 2‐position. 相似文献
156.
Quinolone Analogs 13: Synthesis of Novel 1,1′‐(2‐Methylenepropane‐1,3‐diyl)di(4‐quinolone‐3‐carboxylate) and Related Compounds
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Yoshihisa Kurasawa Kiminari Yoshida Naoki Yamazaki Eisuke Kaji Kenji Sasaki Yoshito Zamami Takatoshi Fujii Min Zhao Hideyuki Ito Haruhiko Fukaya 《Journal of heterocyclic chemistry》2014,51(6):1720-1726
The reaction of the 4‐hydroxyquinoline‐3‐carboxylate 6 with pentaerythritol tribromide gave the 1,1′‐(2‐methylenepropane‐1,3‐diyl)di(4‐quinolone‐3‐carboxylate) 11 , whose reaction with bromine afforded the 1,1′‐(2‐bromo‐2‐bromomethylpropane‐1,3‐diyl)di(4‐quinolone‐3‐carboxylate) 12 . Compound 12 was transformed into the (Z)‐1,1′‐(2‐acetoxymethylpropene‐1,3‐diyl)di(4‐quinolone‐3‐carboxylate) 13 or (E)‐1,1′‐[2‐(imidazol‐1‐ylmethyl)propene‐1,3‐diyl]di(4‐quinolone‐3‐carboxylate) 14 . Hydrolysis of the dimer (Z)‐ 13 or (E)‐ 14 with potassium hydroxide provided the (E)‐1,1′‐(2‐hydroxymethylpropene‐1,3‐diyl)di(4‐quinolone‐3‐carboxylic acid) 15 or (Z)‐1,1′‐[2‐(imidazol‐1‐ylmethyl)propene‐1,3‐diyl]di(4‐quinolone‐3‐carboxylic acid) 16 , respectively. The nuclear Overhauser effect (NOE) spectral data supported that those hydrolysis resulted in the geometrical conversion of (Z)‐ 13 into (E)‐ 15 or (E)‐ 14 into (Z)‐ 16 . 相似文献
157.
158.
159.
A computational algorithm for solving a class of optimal control problems involving terminal and continuous state constraints of inequality type was developed in Ref. 1. In this paper, we extend the results of Ref. 1 to a more general class of constrained time-delayed optimal control problems, which involves terminal state equality constraints as well as terminal state inequality constraints and continuous state constraints. Two examples have been solved to illustrate the efficiency of the method. 相似文献
160.
We study the relationship between the generic smoothness of the Gauss map and the reflexivity (with respect to the projective dual) for a projective variety defined over an algebraically closed field. The problem we discuss here is whether it is possible for a projective variety X in ℙN to re‐embed into some projective space ℙM so as to be non‐reflexive with generically smooth Gauss map. Our result is that the answer is affirmative under the assumption that X has dimension at least 3 and the differential of the Gauss map of X in ℙN is identically zero; hence the projective varietyX re‐embedded in ℙM yields a negative answer to Kleiman–Piene's question: Does the generic smoothness of the Gauss map imply reflexivity for a projective variety? A Fermat hypersurface in ℙN with suitable degree in positive characteristic is known to satisfy the assumption above. We give some new, other examples of X in ℙN satisfying the assumption. (© 2008 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim) 相似文献