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101.
Miwatashi S Arikawa Y Naruo K Igaki K Watanabe Y Kimura H Kawamoto T Ohkawa S 《Chemical & pharmaceutical bulletin》2005,53(4):410-418
A novel series of 4-phenyl-5-pyridyl-1,3-thiazole analogues possessing potent in vitro inhibitory activity against p38 mitogen-activated protein kinase and the release of tumor necrosis factor-alpha (TNF-alpha) from human monocytic THP-1 cells stimulated by lipopolysaccharide has been identified. Subsequent structure-activity relationship (SAR) studies and optimization for absorption, distribution, metabolism, and elimination (ADME) profiles led to the identification of compounds 7 g and 10b as orally active lead candidates that block the in vivo production of proinflammatory cytokine (TNF-alpha). In pharmacokinetic studies, compound 10b showed good oral administration in mice and demonstrated significant in vivo anti-inflammatory activity in an anti-collagen monoclonal antibody-induced arthritis mouse model (minimum effective dose (MED)=30 mg/kg). Further elucidation of this class of compounds may provide novel anti-inflammatory agents, such as anti-rheumatoid arthritis drugs. 相似文献
102.
Three new prenylated butylphloroglucinol derivatives, takaneones A-C (1-3), were isolated from the MeOH extracts of the aerial parts of Hypericum sikokumontanum together with two new prenylated phloroglucinol derivatives, takaneols A and B (4 and 5). The structures of the isolated compounds were elucidated by exhaustive spectroscopic analysis. The cytotoxicities of the isolated compounds against human cancer cell lines were evaluated. Compounds 2-4 showed cytotoxicities against K562/Adr multi-drug resistant (MDR) cancer cells with IC50 values ranging from 4.7 to 10.0 μg/mL, which were slightly more potent than doxorubicin. Their potency of cytotoxicities against MDR cancer cell lines (KB-C2 and K562/Adr) were similar to those against sensitive cell lines (KB and K562). 相似文献
103.
A first synthesis of ascidiacyclamide, a cytotoxic cyclic peptide from ascidian, has been achieved through the cyclodimerization with diphenyl phosphorazidate(DPPA), which has unambiguously determined the absolute configuration of ascidiacyclamide as . 相似文献
104.
Tatsuya Nagae Shunichi Aikawa Koshiro Inoue Yasumasa Fukushima 《Tetrahedron letters》2018,59(45):3988-3993
A colorimetric naked-eye chemosensor for histidine (His) was established by mixing a thiazolylazo dye and Ni2+ in a 1:1?M ratio (TAMSMB-Ni2+). Due to the interaction of Ni2+ with His, TAMSMB was regenerated upon the addition of His to TAMSMB-Ni2+ to lead a significant hypsochromic shift in absorption spectra accompanied by a visual color change from red to yellow which can be directly observed by the naked eye. On the other hands, other amino acids did not trigger any significant changes in absorption properties and solution color. Moreover, it exhibited the selective recognition of His without obvious interference from other amino acids. Thus, TAMSMB-Ni2+ can act as a simple and efficient colorimetric chemosensor for His with sensitivity and selectivity in aqueous solution. 相似文献
105.
The enantioselective formal synthesis of (?)-aurantioclavine is described. The core tricyclic skeleton was synthesized using a Pd-catalyzed Heck insertion–allylic amination cascade. The stereocenter was constructed by a highly enantioselective organocatalytic asymmetric aziridination reaction. 相似文献
106.
The real structure of patellamide A, a cytotoxic lipophilic cyclic peptide from a marine tunicate, has been unambiguously determined by the synthesis of both its proposed and revised structures. 相似文献
107.
Hamada Y 《Chemical & pharmaceutical bulletin》2012,60(1):1-20
2,6-Dimethyl-9-Aryl-9-phosphabicyclo[3.3.1]nonanes (9-PBN and 9-NapBN) and the chiral diaminophosphine oxides (DIAPHOXs) derived from aspartic acid have been introduced as useful ligands and preligands, respectively, for transition metal-catalyzed asymmetric synthesis. anti-Selective asymmetric hydrogenation of α-amino-β-ketoesters using Ru-, Rh-, Ir-, and Ni-catalysts through dynamic kinetic resolution have been developed for the first time, producing efficiently important anti β-hydroxy-α-amino acids. The total synthesis of several biologically active natural products was achieved by use of the transition metal-catalyzed reaction using DIAPHOX, anti-selective asymmetric hydrogenation, and reactions developed by us. Synthesis of tangutorine, an antitumor indole alkaloid, has been enantioselectively achieved for the first time. Enantioselective synthesis of a martinelline chiral core was accomplished using the asymmetric tandem Michael-Aldol reaction as a key step developed by us. This synthesis represents the formal total synthesis of martinelline and martinellic acid. Papuamide B was synthesized through the elucidation of unknown stereostructures by using the anti-selective asymmetric hydrogenation and reactions developed by us. 相似文献
108.
Ken-ichi Yamada Yasumasa Matsumoto Khalid B. Selim Yasutomo Yamamoto Kiyoshi Tomioka 《Tetrahedron》2012,68(22):4159-4165
Steric tuning of C2-symmetric chiral N-heterocyclic carbene (NHC) was performed in Au(I)-catalyzed asymmetric cyclization of 1,6-enyne. Higher enantioselectivity was realized when chiral NHC–AuCl/AgSbF6 catalysts whose N-substituent on the NHC overlays the Au–Cl bond was utilized. 相似文献
109.
We developed a novel asymmetric synthetic method for multisubstituted 9,10-dihydrophenanthrenes based on the Pd-catalyzed asymmetric intramolecular Friedel-Crafts allylic alkylation of phenols, which produces 10-vinyl or 10-isopropenyl chiral 9,10-dihydrophenanthrene derivatives in high yield with up to 94% ee. 相似文献
110.
A parametric loudspeaker radiates an audible signal by the interaction of the primary wave that is amplitude modulated and is known as a super-directivity loudspeaker. The parametric loudspeaker is one of the prominent applications of nonlinear acoustics. So far, the applications have been limited monaural reproduction sound system for public address in museum, station, street etc. In this paper, we investigated sound localization of stereo reproduction using two parametric loudspeakers in comparison with that using two ordinary dynamic loudspeakers. In subjective tests, the binaural information ILD (Interaural Level Difference) or ITD (Interaural Time Delay) was focused on. To investigate the characteristics of sound localization in a wide listening area, three typical listening positions were picked up. Signals were 500 Hz, 1 kHz, 2 kHz and 4 kHz pure tones and pink noise. The used parametric loudspeaker was an equilateral hexagon. The subjective test led to the results that when the parametric loudspeakers were used, the listeners at the three typical listening positions perceived the correct sound localization of not only pure tone but also pink noise and when the ordinary dynamic loudspeakers were used, except for the case of pure tone with ITD, the tendency was almost similar to those using the parametric loudspeakers. The second subjective tests were conducted in order to investigate in details the difference between parametric loudspeakers and ordinary dynamic loudspeakers by increasing the number of subjects. In the case of ITD and 500 Hz using the ordinary dynamic loudspeakers, three types of sound localization were categorized, in which the reversed type was major and the normal and the other types were minor. The ILDs which were measured with a dummy head and were calculated with several formulas were almost the same and indicated the reasons of the reversed typed sound localization and a serious influence of the crosstalk. It was found that in the case of pure tone with ITD, the contradiction between the binaural information ILD and ITD is remarkable, because the directivity of the ordinary dynamic loudspeakers was so dull that the crosstalk components had a serious influence on sound localization. It was determined the parametric loudspeaker could transmit correct binaural information to the listener, because the directivity of the parametric loudspeakers was so sharp that it suppressed the cross talk components. 相似文献