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Ogawa T Araki M Miyamae T Okayama T Hagiwara M Sakurada S Morikawa T 《Chemical & pharmaceutical bulletin》2003,51(7):759-771
To improve the oral bioavailability of a dermorphin tetrapeptide analog, N(alpha)-1-iminoethyl-Tyr-D-MetO-Phe-MebetaAla-OH (III), which has a potent analgesic activity after oral administration, various derivatives were synthesized to increase lipophilicity by esterification of the C-terminal carboxyl group and/or acylation of the phenolic hydroxyl group on Tyr1. Antinociceptive activity was evaluated after subcutaneous or oral administration using the mouse tail pressure test. As a result, increased antinociceptive activity after oral administration as well as an improved ED50(p.o.)/ED50(s.c.) ratio, which is an indicator of oral bioavailability, were found for some compounds. With regard to the improvement of bioavailability, derivatives with acylation of the phenolic hydroxyl group on Tyr1 showed better results than derivatives with esterification of the C-terminal carboxyl group. In particular, an ED50(p.o.)/ED50(s.c.) ratio equivalent to that of morphine was found for an acetylated derivative, N(alpha)-1-iminoethyl-Tyr(COMe)-D-MetO-Phe-MebetaAla-OH (7a), as well as for a methoxycarbonylated derivative, N(alpha)-1-iminoethyl-Tyr(CO2Me)-D-MetO-Phe-MebetaAla-OH (7l). 相似文献
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Takeshi Nishii Fumiaki Miyamae Makoto Yoshizuka Hiroto Kaku Mitsuyo Horikawa Makoto Inai Tetsuto Tsunoda 《Tetrahedron: Asymmetry》2012,23(10):739-741
Excess lithium hexamethyldisilazide (LHMDS) with LiCl prompted the asymmetric aza-Claisen rearrangement of carboxamide and retarded the decomposition of its amide enolate. The addition of these two reagents was a key step that led to the total synthesis of (+)-α-cuparenone with a stereogenic quaternary center. 相似文献
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Masahiro Yamashita Daisuke Kawakami Satoshi Matsunaga Yoshio Nakayama Mari Sasaki Shinya Takaishi Fumiyasu Iwahori Hitoshi Miyasaka Ken‐ichi Sugiura Yoshiki Wada Hiroshi Miyamae Hiroyuki Matsuzaki Hiroshi Okamoto Hisaaki Tanaka Kazuhiro Marumoto Shin‐ichi Kuroda 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2004,116(36):4867-4871
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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
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Decomposition of Benzene in Air in a Plasma Reactor: Effect of Reactor Type and Operating Conditions 总被引:2,自引:0,他引:2
Ogata A. Miyamae K. Mizuno K. Kushiyama S. Tezuka M. 《Plasma Chemistry and Plasma Processing》2002,22(4):537-552
The decomposition of benzene was carried out in two types of plasma reactors packed with BaTiO3 pellets: one reactor had two stainless steel electrodes (SUS reactor), and the other reactor had a glass layer between two concentric electrodes (GL reactor). The decomposition efficiency and the suppression of formation of N2O and NOx were greater in the GL reactor than in the SUS reactor. In contrast, the suppression of O3 formation and the oxidation to COx in the SUS reactor were superior to those in the GL reactor. The effect of wa eform and frequency of applied ac power was in estigated for each reactor. 相似文献
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Ogawa A Miyamae Y Honma A Koyama T Yazawa K Shigemori H 《Chemical & pharmaceutical bulletin》2011,59(5):672-675
A new compound, pycnalin (1), together with four known compounds, ginnalins A (2), B (3), C (4), and 3,6-di-O-galloyl-1,5-anhydro-D-glucitol (3,6-di-GAG) (5), were isolated from Acer pycnanthum. The structure of 1 was determined on the basis of 2D-NMR spectral data and synthesis of 1. Pycnalin (1) is the first 1,5-anhydro-D-mannitol linked to a gallic acid, while compounds 2-5 were 1,5-anhydro-D-glucitol linked to gallic acids. All compounds were tested in vitro for α-glucosidase inhibitory and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities. Pycnalin (1) exhibited moderate α-glucosidase inhibitory activity as well as free radical scavenging activity. Ginnalin A (2) and 3,6-di-GAG (5), which have two galloyl groups, exhibited potent α-glucosidase inhibition, compared to those of other compounds 1, 3, and 4 containing a galloyl group. These results suggest that α-glucosidase inhibition is influenced by the number of galloyl groups. 相似文献
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