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T Yamakawa H Matsukura Y Nomura M Yoshioka M Masaki H Igata S Okabe 《Chemical & pharmaceutical bulletin》1991,39(7):1746-1752
A series of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines (3) was synthesized and evaluated for its biological activity against gastric H+/K(+)-ATPase prepared from rabbit stomach and gastric acid secretions in Heidenhain pouch dogs. Monoalkyl substituents on the nitrogen atom of the aniline moiety markedly inhibited the enzyme activity to the same degree as omeprazole, a representative H+/K(+)-ATPase inhibitor. Most of these compounds, administered at 3 mg/kg i.v. inhibited histamine-stimulated gastric acid secretion. The inhibitory activity of these derivatives on the enzymes at pH 6.0 was more potent than that at pH 7.4, and was distinctly correlated to stability in aqueous solution at pH 5.0. 相似文献
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The percutaneous absorption of ketoprofen (KPF) from gel patches containing d-limonene and ethanol was investigated in rats. Plasma levels of KPF varied with the kind of polymers which constitute the gel patch, and the highest level was observed when the copolymer of ethylacrylate (EA) and diethyleneglycolmethacrylate (DEGMA) was used as a vehicle. The amount of KPF permeating through the rat skin from the gel patch was well correlated with that of ethanol. Permeations were enhanced with increase in the amount of d-limonene distributed from the vehicle to the skin tissue. The amount of d-limonene accumulated in the skin varied greatly with the kind of polymers; the highest accumulation was observed with the EA-DEGMA copolymer, and decreased with increasing affinity of d-limonene to the polymers. The reason EA-DEGMA copolymer showed the highest percutaneous absorption of KPF from gel patches containing d-limonene may be the hydrophilic nature of this polymer which showed the lowest affinity to d-limonene. 相似文献
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Hiroshi Maruoka Kenji Yamagata Fumi Okabe Yukihiko Tomioka 《Journal of heterocyclic chemistry》2005,42(4):717-721
A series of cyclic sulfonium ylides 4a‐h reacted with titanium( IV ) chloride in the presence of triethyl‐amine to give the corresponding fused 2,3‐dihydro‐1H‐thieno[3,4‐b]pyrroles 5a‐h , via a ring opening and recyclization. In contrast, treatment of compounds 4a, 4b, 4e and 4f with titanium(IV) chloride, triethy‐lamine and dimethylamine hydrochloride gave the corresponding thiophenes 6a, 6b, 6e and 6f . Furthermore, compounds 6a and 6b easily underwent cyclization with sodium hydride to afford the corresponding 5a and 5b . 相似文献
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Kashiwada Y Chiyo J Ikeshiro Y Nagao T Okabe H Cosentino LM Fowke K Morris-Natschke SL Lee KH 《Chemical & pharmaceutical bulletin》2000,48(9):1387-1390
3-Alkylamido-3-deoxy-betulinic acids were synthesized and evaluated for anti-HIV activity as part of the structure-activity relationship study of the potent anti-HIV agent 3-O-(3',3'-dimethyl)-succinyl-betulinic acid (DSB) (2). 3Alpha-diglycorylamide-3-deoxy-betulinic acid demonstrated relatively potent anti-HIV activity (EC50 0.24 microm, TI 728). However, replacing the ester group at C-3 in 2 and its analogues with an amido group yielded inactive or much less potent compounds against HIV replication, indicating that the ester group at C-3 in 2-4 is essential for potent anti-HIV activity. 相似文献
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Mingdeng Wei Kiyomi Okabe Hironori Arakawa Yesutake Teraoka 《Reaction Kinetics and Catalysis Letters》2002,77(2):381-387
SiO2 was modified by hexagonal mesoporous silica to form a mixture with meso-/macroporous sizes and used as support of Co catalysts for Fischer-Tropsch synthesis in a slurry phase. A synergistic effect on the activity of Co catalyst was found. The catalytic properties are related to the state of surface Co and the character of support. 相似文献
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Carbodithioic acids react with trivalent sulphur compounds bearing semipolar linkages (sulphoxides, sulphonium ylides and sulphilimines), to give the corresponding sulphides and add to olefins to afford dithioesters. The orientation of olefin addition is controlled by the olefin nature. Michael type addition takes place with olefins bearing an electron-withdrawing group α to the double bond while Markownikoff addition occurs with olefins bearing an electron-donating group. With vinyl and allyl sulphoxides, both addition and reduction took place simultaneously, and new dithioesters were obtained. 相似文献
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Narisawa Masaki Okabe Yoshio Iguchi Masahiro Okamura Kiyohito Kurachi Yasuo 《Journal of Sol-Gel Science and Technology》1998,12(3):143-152
Inorganic-organic hybrid gels were prepared by simultaneous condensation of the liquid mixture of ethyl silicate, ethyl borate and water soluble phenol resin with low molecular weight. The liquid mixtures were changed into lightly colored transparent gels after a catalyst addition and stirring. The obtained gels were crushed, dried and fired in controlled conditions to yield the inorganic precursors. Since the tailored inorganic precursors mainly consisted of SiO2 and carbon, silicon carbide was formed with the heat treatments in an Ar atmosphere beyond 1773 K with carbothermic reduction. The properties and morphology of the formed silicon carbide powders in terms of the starting precursor compositions and the conditions of the carbothermic reduction were investigated with SEM, XRD and TG-DTA analysis. 相似文献
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