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51.
Tatsuro Ouchi Toshio Banba Hiroshi Masuda Tatsuji Matsumoto Shigeo Suzuki Masuko Suzuki 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(10):959-975
In order to provide a macromolecular prodrug of 5-fluorouracil (5FU) reducing the side effects, having an affinity for tumor cells, and exhibiting strong antitumor activity, the covalent attachments of 5FUs to chitosan and chitosamino-oligosaccharide (COS) through hexamethylene spacer groups via urea, urea bonds were carried out. The effect of prolongation of life was tested in vivo against p388 lyrnphocytic leukemia in female CDF, mice by intra-peritoneal (i.p.) transplantation/i.p. injection and the growth-inhibitory effect on Meth-A fibrosarcoma or MH-134Y heputoma was evaluated in vivo in SPF-C3H/He scl male or Balb/c male mice by subcutaneous (s.c.) implantation/intravenous (i.v.) injection. The effects of the degree of polymerization of chitosan and 相似文献
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Synthesis of 3,3′-(1,6-hexanediyl)bis-pyrimidine derivatives and 3,4-dithia[6.6](1.3)pyrimidinophane
Toshio Kinoshita Shirou Odawara Keiko Fukumura Sunao Furukawa 《Journal of heterocyclic chemistry》1985,22(6):1573-1576
Several 3,3′-(1,6-hexanediyl)bis[6-methyl-2,4(1H,3H)-pyrimidinedione] derivatives ( 4a, 4b , and 4c ) were synthesized from 1,6-(hexanediyl)bis[6-methyl-2H-1,3-oxazine-2,4(3H)-dione] (3) . Compound 4c was converted to 6, which reacted with thiourea giving thiuronium salt 7 . 3,3′-(1,6-Hexanediyl)bis [1-(2-mercaptoethyl)-6-methyl-2,4(1H,3H)-pyrimidinedione] (9) was obtained by the hydrolysis of 7 , and then 9 was oxidized to 12,22-dimethyl-3,4-dithia[6.6] (1.3)-1,2,3,4-tetrahydro-2,4-dioxopyrimidinophane (10) . 相似文献
54.
Miura H Kanebako M Shirai H Nakao H Inagi T Terada K 《Chemical & pharmaceutical bulletin》2011,59(6):686-691
The physicochemical characteristics and oral absorption of a poorly water-soluble drug, K-832, adsorbed onto porous silica (Sylysia 350), were compared with those of K-832 adsorbed onto non-porous silica (Aerosil 200). K-832 and silica were treated with supercritical CO(2) (scCO(2)) to produce K-832-Sylysia 350 and K-832-Aerosil 200 formulations. Scanning electron microscopy, polarizing microscopy, powder X-ray diffraction, and differential scanning calorimetry results suggested that K-832 mainly existed in an amorphous state in both formulations. The specific surface area of both formulations was much larger than that of pure K-832 crystals. The dissolution rate of K-832 from both formulations was considerably greater than that from corresponding physical mixtures due to rapid wetting of the hydrophilic carrier surfaces and amorphous state, the dissolution from the K-832-Sylysia 350 formulation being the fastest. In vivo absorption tests on the two formulations indicated no significant differences in their peak concentration (C(max)) and the area under their plasma concentration-time curve (AUC), while the concentrations of K-832 in the K-832-Sylysia 350 formulation were significantly higher than those in the K-832-Aerosil 200 formulation 1 h and 1.5 h after administration of these formulations (p<0.05). This could be attributed to the different dispersion states of K-832 in the formulations due to their different three-dimensional structures (porous and non-porous). In physical stability tests, the amorphous drugs in both formulations were stable at room temperature for at least 14 months. Thus, the absorption of poorly water-soluble drugs could be greatly improved by adsorption onto porous silica using scCO(2). 相似文献
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Sako M Kihara T Tanisaki M Maki Y Miyamae A Azuma T Kohda S Masugi T 《The Journal of organic chemistry》2002,67(3):668-673
The UV irradiation of pyrrolnitrin (1a), which is an antibiotic clinically useful against dermatophytosis and possesses a unique 2-(pyrrol-3-yl)nitrobenzene moiety in the molecule, in an anhydrous aprotic solvent resulted in the exclusive formation of transient 7,4'-dichlorospiro[1,3-dihydrobenzo(c)isoxazole-3,3'-pyrrolin-2'-one] (2a) via the intramolecular oxidation of the juxtaposed pyrrole ring by the triplet-excited nitro group. The irradiation in an aqueous aprotic solvent, however, allowed the concurrent occurrence of intramolecular cyclization by the singlet-excited nitro group in 1a and the hydroxylation at the 2-position of the pyrrole ring by water to afford 3,7-dichloro-8-hydroxy-8,8a-dihydropyrrolo[2,3-b]indol-2-one (3a), accompanied by the formation of 2a. Elongation of the irradiation time in these photoreactions caused a rapid consumption of the products, 2a and 3a, to give undetermined polar polymeric products. The present results indicate that the photodegradation of 1a is significantly influenced by the presence of water in the reaction media and by the nature of its excited state. Thus, the loss of the antifungal activities by the photosensitive antibiotic 1a was chemically proved. 相似文献
57.
Polymerization of N-carbazolylacetylene by various transition metal catalysts and polymer properties
Tomoaki Sata Ryoji Nomura Tatsuo Wada Hiroyuki Sasabe Toshio Masuda 《Journal of polymer science. Part A, Polymer chemistry》1998,36(14):2489-2492
N-Carbazolylacetylene (CzA) was polymerized in the presence of various transition metal catalysts including WCl6, MoCl5, [Rh(NBD)Cl]2, and Fe(acac)3 to give polymers in good yields. The polymers produced with W catalysts were dark purple solids and soluble in organic solvents such as toluene, chloroform, etc. The highest weight-average molecular weight of poly(CzA) reached about 4 × 104. In the UV–visible spectrum in CHCl3, poly(CzA) exhibited an absorption maximum around 550 nm (εmax = 4.0 × 103 M−1 cm−1) and the cutoff wavelength was 740 nm, showing a large red shift compared with that of poly(phenylacetylene) [poly(PA)]. Poly(CzA) began to lose weight in TGA under air at 310°C, being thermally more stable than poly(PA) and poly[3-(N-carbazolyl)-1-propyne]. Poly(CzA) showed a third-order susceptibility of 18 × 10−12 esu, which was 2 orders larger than that of poly(PA). © 1998 John Wiley & Sons, Inc. J. Polym. Sci. A Polym. Chem. 36: 2489–2492, 1998 相似文献
58.
Tsuneyuki Sato Toshio Kadowaki Hiroshi Takeda Takayuki Otsu 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(8):1225-1239
(S)-4-Methyl-2-N,N-dimethylaminopentyl methacrylate (DMAPM) was synthesized from the reaction of N,N-dimethyl-L-leucinol with methacryl chloride, and its radical polymerization was investigated. It was found that DMAPM readily polymerized by α,α1-azobisisobutyronitrile (AIBN) as an initiator to give poly-DMAPM. The copolymerization of DMAPM(M1) with styrene(Mz) was also studied in various solvents with AIBN as an initiator at 60°C. From the result obtained in benzene, Q and e values of DMAPM were determined to be 0.64 and -0.04, respectively. Specific rotations of the copolymers of DMAPM with styrene were not proportional to the weight percent of the DMAPM unit incorporated, but the observed relation gave a downward curve. The copolymerizations DMAPM with α, β-disubstituted monomers such as maleic acid, maleimide, and N-phenylmaleimide were carried out in order to induce asymmetric center in the polymer chain. After hydrolysis of the copolymers obtained, the hydrolyzed polymers were found to be optically active, suggesting an induction of asymmetric center into the polymer chain. 相似文献
59.
Propylene was polymerized with the catalyst system (C2H5)2A1C1/ VCk/ anisole at -78°C using various conditions. The resulting polymers were successively extracted by diethyl ether, hexane, and heptane, leaving the residue. The polymers of the four series were characterized by intrinsic viscosity, gel permeation chromatography, 13C nuclear magnetic resonance, infrared spectroscopy, x-ray diffraction, and by differential scanning calorimetry. The combined evidence from the various methods indicates that this catalyst system leads to stereoblock polymers which can be fractionated according to stereochemical composition and sequence length. 相似文献
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