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21.
22.
Tobe M Isobe Y Tomizawa H Nagasaki T Aoki M Negishi T Hayashi H 《Chemical & pharmaceutical bulletin》2003,51(9):1109-1112
We investigated the chemical modifications of the nitroquinazoline derivative (1) through the replacement of the NH group at the C(4)-position with several N-alkyl groups to increase the lipophilicity at the C(4)-position. Among them, we found that the N-methyl analogue (5a) showed a 2-fold loss in the inhibitory activity toward tumor necrosis factor-alpha (TNF-alpha) production in vitro as compared with the NH analogue (1); however, 5a exhibited an oral inhibitory activity on TNF-alpha production with an ED50 value of 26 mg/kg, whereas 1 did not. Moreover, the oral bioavailability of 5a was higher than that of 1 (1, F=1%; 5a, F=21%), and the calculated ClogP value for 5a was higher than that for 1. These results suggest that the improved lipophilicity of 5a compared with that of 1 reflects its greater inhibitory activity on TNF-alpha production in vivo as well as oral bioavailability. 相似文献
23.
We have developed an ultrasonic micro-motor for use as a micro-actuator in place of an electromagnetic motor. This ultrasonic micro-motor, which can be driven by a single signal and in which the change of the direction of the rotor movement can be made easily by selecting the electrode to apply the driving signal, can easily construct a self-oscillating circuit and simplify the driving circuit. We have also simplified the motor structure, which is easy to miniaturize and mass-produce. We applied a version of this motor with a diameter of 8 mm to a vibration alarm, and one with a diameter of 4.5 mm to a driving source of a calendar mechanism in a watch. This ultrasonic micro-motor is expected to be of use as a new driving source in a broad range of fields. 相似文献
24.
We demonstrate the nanosecond time-gated spectroscopy of plume luminescence in UV laser ablation of human hair. Clear and sharp peaks of calcium ion (Ca+) appear in the spectrum although the Ca content is only 0.1% in human hair. Highly sensitive detection of Ca is thus possible. In the experiment, the peak intensity of Ca+ was measured for human hair samples of female subjects over a wide range of age, and compared to the bone mineral density of the lumbar vertebrae of the subjects themselves. Our experimental results suggest that this specific spectroscopy has the potential for novel diagnoses including monitoring of daily Ca intake and a screening diagnosis of osteoporosis. The spectroscopic system and time transition of plume-luminescence spectra are also described. 相似文献
25.
Takashi Yoshida Rong Lu Shuqin Han Kazuyuki Hattori Takahiro Katsuta Kei‐Ichi Takeda Kazutoshi Sugimoto Masamitsu Funaoka 《Journal of polymer science. Part A, Polymer chemistry》2009,47(3):824-832
For the synthesis of a new biologically functional polymer from a natural resource by an environment‐friendly method, the laccase‐catalyzed polymerization of a lignin‐based macromonomer, lignocatechol, was carried out for the first time in ethanol–phosphate buffer solvent system to give crosslinked polymers in good yields. Lignocatechol was prepared by the phase separation system of lignin and catechol in aqueous sulfuric acid. The copolymerization was also performed with urushiol to afford the corresponding copolymers in high yields. The polymerization mechanism was estimated by the IR and pyrolysis GC‐MS measurements, suggesting that the polymerization proceeded mainly at the catechol ring through a quinone radical intermediate. The thermal properties were measured by the DSC, TG, and TMA analyses, indicating that the polymers had high thermal stabilities because of the crosslinked structures. In addition, it was found that the resulting polymers had the affinity of bovine serum albumin (BSA) and glucoamylase. © 2008 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 47: 824–832, 2009 相似文献
26.
Nobuhiro Kihara Yusuke Iino Tatsuya Misawa 《Journal of polymer science. Part A, Polymer chemistry》2008,46(18):6255-6262
The condensation polymerization of isophthalodihydrazide and diphenyl isophthalate affords poly(isophthaloylhydrazine‐1,2‐diyl). High‐molecular‐weight poly(5‐tert‐butylisophthaloylhydrazine‐1,2‐diyl) is prepared by the polycondensation of 5‐tert‐butylisophthalodihydrazide and bis(4‐nitrophenyl) 5‐tert‐butylisophthalate in NMP at 100 °C. Td of the poly(diacylhydrazine) is observed above 300 °C. No Tg is observed below Td. The high‐molecular‐weight poly(diacylhydrazine) exhibits a film‐forming ability. The poly(diacylhydrazine) decomposes on treatment with an oxidant such as sodium hypochlorite solution to obtain the corresponding carboxylic acid and nitrogen. However, poly(diacylhydrazine) was stable to oxygen and hydrogen peroxide even in the presence of transition metal ions. © 2008 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 46: 6255–6262, 2008 相似文献
27.
Takashi Tokoroyama Masamitsu Tsukamoto Toshihiro Asada Hideo Iio 《Tetrahedron letters》1987,28(52):6645-6648
Doubly stereocontrolled cyclization of the allylsilane derivative 1 followed by trapping of the enolate with ClCH2SMe gives in one-pot manner the decalone derivatve 5 in which all of the four contiguous diastereomeric centers of
-clerodane skeleton have been secured. The total synthesis of linaridial 4 have been accomplished from 5. 相似文献
28.
Non-extractable photoinitiators based on thiol-functionalized benzophenones and thioxanthones 总被引:1,自引:0,他引:1
Hironori Matsushima Qin Li Masamitsu Shirai Charles E. Hoyle 《European Polymer Journal》2010,46(6):1278-1287
Non-extractable photoinitiators could be advantageous for use in biological, electronic, and food packaging applications. Therefore, thioxanthone and benzophenone derivatives were synthesized from 1,6-hexane dithiol and chlorinated benzophenone or thioxanthone. The efficiency of thiol-functionalized photoinitiators in combination with amine co-initiators was compared to benzophenone and isopropylthioxanthone with amine co-initiators, and the cleavage of photoinitiator 2,2-dimethoxy-1,2-diphenylethan-1-one in acrylic resins. The reaction kinetics were analyzed using photo-differential scanning calorimetry and real-time FTIR. Coating physical properties were evaluated by pendulum and pencil hardness, steel-wool scratch and mandrel bend tests. The non-extractable photoinitiators had higher absorbance than their benzophenone or isopropylthioxanthone counterparts due to the sulfide substitution on the phenyl ring, and the free thiol groups reacted with the acrylate by either an amine catalyzed Michael addition or a free-radical chain process. The combination of thiol-functionalized photoinitiators with secondary amines provides an efficient photoinitiator system that is locked into the photopolymerized network and cannot be extracted with typical solvents. 相似文献
29.
Sakihito Kitajima Kaeko Kamei Shigeru Taketani Masamitsu Yamaguchi Fumiko Kawai Aino Komatsu Yoshihiro Inukai 《BMC biochemistry》2010,11(1):6
Background
Plant latex is the cytoplasm of highly specialized cells known as laticifers, and is thought to have a critical role in defense against herbivorous insects. Proteins abundantly accumulated in latex might therefore be involved in the defense system. 相似文献30.
Katsuhiko Takenaka Natsuyo Shibata Akihiko Oshikiri Masamitsu Miya Hiroki Takeshita Tomoo Shiomi 《Journal of polymer science. Part A, Polymer chemistry》2010,48(17):3714-3721
Anionic polymerizations of three 1,3‐butadiene derivatives containing different N,N‐dialkyl amide functions, N,N‐diisopropylamide (DiPA), piperidineamide (PiA), and cis‐2,6‐dimethylpiperidineamide (DMPA) were performed under various conditions, and their polymerization behavior was compared with that of N,N‐diethylamide analogue (DEA), which was previously reported. When polymerization of DiPA was performed at ?78 °C with potassium counter ion, only trace amounts of oligomers were formed, whereas polymers with a narrow molecular weight distribution were obtained in moderate yield when DiPA was polymerized at 0 °C in the presence of LiCl. Decrease in molecular weight and broadening of molecular weight distribution were observed when polymerization was performed at a higher temperature of 20 °C, presumably because of the effect of ceiling temperature. In the case of DMPA, no polymer was formed at 0 °C and polymers with relatively broad molecular weight distributions (Mw/Mn = 1.2) were obtained at 20 °C. The polymerization rate of PiA was much faster than that of the other monomers, and poly(PiA) was obtained in high yield even at ?78 °C in 24 h. The microstructure of the resulting polymers were exclusively 1,4‐ for poly(DMPA), whereas 20–30% of the 1,2‐structure was contained in poly(DiPA) and poly(PiA). © 2010 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 48: 3714–3721, 2010 相似文献