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71.
72.
Shuichi Oi Mitsutoshi Moro Hiroe Fukuhara Takanori Kawanishi Yoshio Inoue 《Tetrahedron letters》1999,40(52):9259-9262
A rhodium complex catalyzed the addition of aryl- and alkenyl-stannanes to activated aldimines under mild and neutral conditions, affording the corresponding amines in good yields. 相似文献
73.
[reaction: see text] In the reaction of p-chlorophenyl alkyl sulfides with IF(5), polyfluorination reaction took place on the alkyl chain with the migration of the arylthio group. Consequently, p-chlorophenyl polyfluoroalkyl sulfides, having 3-7 fluorine atoms depending on alkyl chain length, could be obtained selectively. 相似文献
74.
Kaneko T Clark RS Ohi N Ozaki F Kawahara T Kamada A Okano K Yokohama H Ohkuro M Muramoto K Takenaka O Kobayashi S 《Chemical & pharmaceutical bulletin》2004,52(6):675-687
Novel piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4]benzothiazine were prepared and evaluated for their inhibitory activity on the upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1). Replacement of the methanesulfonyl group on the piperidine ring of previously prepared derivatives with a carboxylic acid-containing moiety resulted in a number of potent adhesion molecule inhibitors. Of these, (anti) [3-(10H-pyrazino[2,3-b][1,4]benzothiazin-8-yl)methyl-3-azabicyclo[3.3.1]non-9-yl]acetic acid 2q (ER-49890), showed the most potent oral inhibitory activities against neutrophil migration in an interleukin-1 (IL-1) induced paw inflammation model using mice, and leukocyte accumulation in a carrageenan pleurisy model in the rat, and therapeutic effect on collagen-induced arthritis in rats. 相似文献
75.
Hanqiao Xu Dr. Takashi Kurohara Reina Takano Dr. Hidetomo Yokoo Dr. Norihito Shibata Dr. Nobumichi Ohoka Dr. Takao Inoue Prof. Mikihiko Naito Dr. Yosuke Demizu 《ChemistryOpen》2022,11(7):e202200131
Optimizing linker design is important for ensuring efficient degradation activity of proteolysis-targeting chimeras (PROTACs). Therefore, developing a straightforward synthetic approach that combines the protein-of-interest ligand (POI ligand) and the ligand for E3 ubiquitin ligase (E3 ligand) in various binding styles through a linker is essential for rapid PROTAC syntheses. Herein, a solid-phase approach for convenient PROTAC synthesis is presented. We designed azide intermediates with different linker lengths to which the E3 ligand, pomalidomide, is attached and performed facile PROTACs synthesis by forming triazole, amide, and urea bonds from the intermediates. 相似文献
76.
Ghiani S Baroni S Burgio D Digilio G Fukuhara M Martino P Monda K Nervi C Kiyomine A Aime S 《Magnetic resonance in chemistry : MRC》2008,46(5):471-479
Melanin granules (MGs) have been extracted from human Chinese black hairs by either acid hydrolysis (CH-type MGs) or enzymatic digestion (CP-type MGs), and their chemical structure investigated at the solid state by means of (13)C cross polarization magic angle spinning (CPMAS NMR) and EPR spectroscopy. Both types of MGs contain a large amount of protein that is tightly bound to the true melanin polymer, with CP-type MGs having a larger protein content than CH-type ones. Moreover, MGs may also contain variable amounts of lipid-like material. A high amount of paramagnetic metals is detected by EPR in CP-type MGs, in particular Fe(III). Iron can be bound in two chemical forms: as isolated high spin Fe(III) ions with rhombic symmetry and as small oxy-hydroxy Fe(III) aggregates. Iron is poorly available to chelators. CH-type MGs contain much fewer metals. CP-type MGs have then been subjected to partial bleaching by hydrogen peroxide in ammonia, yielding a residual solid, called residual oxidized melanin (ROM) and a soluble but still pigmented fraction called melanin free acid (MFA). MFA can be isolated by precipitation at acidic pH. The (13)C-CPMAS NMR and EPR spectra of these derivatives indicated that ROM has a structure very similar to that of parent MGs, whereas MFA shows a decrease of the protein content with respect to the melanin and a decreased amount of bound iron. Thus, the oxidative degradation of CP-type MGs is a process not involving the bulk of MGs, but rather it proceeds from the solvent-exposed outer parts to the interior. 相似文献
77.
In contrast to the photosensitization with a non-methylated analogue, supramolecular photochirogenesis with a novel permethylated mono(6-O-benzoyl)-beta-cyclodextrin exhibited a critical dependence of the product's enantiomeric excess upon temperature, and possessed a large differential entropy of activation (-11 J K(-1) mol(-1)) for which the flexible host skeleton is likely to be responsible. 相似文献
78.
Montfrooij W Aronson MC Rainford BD Mydosh JA Murani AP Haen P Fukuhara T 《Physical review letters》2003,91(8):087202
We present inelastic neutron scattering experiments, performed near the antiferromagnetic quantum critical point in Ce(Ru0.24Fe0.76)2Ge2. Both local and long-range fluctuations of the local moments are observed, but due to the Kondo effect only the latter are critical. We propose a phenomenological expression which fits the energy E, temperature T, and wave vector q dependences of the dynamic susceptibility, describing the non-Fermi liquid E/T scaling found at every q. 相似文献
79.
Nakanishi I Nishizawa C Ohkubo K Takeshita K Suzuki KT Ozawa T Hecht SM Tanno M Sueyoshi S Miyata N Okuda H Fukuzumi S Ikota N Fukuhara K 《Organic & biomolecular chemistry》2005,3(18):3263-3265
Photoreduction of pyridine N-oxide, which has a key structure of antitumor agents for hypoxic solid tumors, by 1-benzyl-1,4-dihydronicotinamide in deaerated aprotic media resulted in generation of hydroxyl radical, leading to the oxidation of salicylic acid to 2,3- and 2,5-dihydroxybenzoic acids, and catechol. 相似文献
80.