最新巻号

後続誌

Chemical and Pharmaceutical Bulletin

巻号一覧
Pharmaceutical Bulletin
- Vol.5(1957)
- Vol.4(1956)
- Vol.3(1955)
- Vol.2(1954)
- Vol.1(1953)

Pharmaceutical Bulletin Vol. 5(1957) No. 6

Biochemical Studies on Pathogenic Fungi. VI. Nutritional Studies on Trichophyton gypseum with Special Reference to its Pleomorphism.

藤井達三

公開日: 2008年02月19日

P503-506

Carbohydrate utilization and nitrogen requirement of Trichophyton gypseum were studied and differences in the nutritional physiology between the normal and pleomorphic forms of this fungus were demonstrated. The pleomorphic form showed better growth and more efficient assimilation on monosaccharides than the normal form. Dior polysaccharides generally failed to support appreciable growth of either form. The pleomorphic form grew far more readily on single amino acid than the normal form, and reproduced even on ammonium nitrogen to some extent which the normal form could not utilize at all.

Biochemical Studies on Pathogenic Fungi. VII. The Effect of Synthetic Fungicides and Fatty Acids on the Respiration of Trichophyton gypseum.

藤井達三

公開日: 2008年02月19日

P506-510

The effect of synthetic fungicides and fatty acids on the respiration of normal and pleomorphic forms of Trichophyton gypseum was examined manometrically. Organic thiomercuric fungicides, cationic detergents, and undecylenic acid markedly inhibited the respiration in as low as 10^-3 to 10^-5 molar concentration. Close relationship was observed between their respiration- and growth-inhibiting effects. The pleomorphic form was much more sensitive to the action of these compounds than the normal form of this fungus. Every saturated fatty acid of even-numbered series from C₂ to C₁₆ stimulated the respiratory rate of this fungus in a certain range of concentrations, while higher members among them above C₈ inhibited it in relatively higher concentration. The inhibitory action was stronger in the undissociated state than as anion of the same acid, and was the maximum with the C₁₂ acid. This dermatophyte was more sensitive to the action of these acids than bacterial species examined.

Biochemical Studies on Pathogenic Fungi. VIII. The Effect of an Antibiotic, Trichomycin, on the Respiration and Phosphorus Metabolism of Trichophyton gypseum.

藤井達三

公開日: 2008年02月19日

P511-514

The action of Trichomycin on the respiration and phosphorus metabolism of Trichophyton gypseum was examined. This antibiotic stimulated the respiratory rate of this fungus in a range of 0.1∼100γ/cc., while it inhibited the rate markedly over 100γ/cc. The inhibitory action of Trichomycin upon the incorporation of phosphate into the cells from the surrounding medium was demonstrated with the aid of ³²P-labeled phosphate. Such an effect appeared from 0.1γ/cc.

Naphthoresorcinol Picrate for the Determination of Glucuronic Acid in Physiological Materials.

石館守三, 南原利夫

公開日: 2008年02月19日

P515-518

Naphthoresorcinol picrate, 1 : 1 molecular compound, is recommended for the microdetermination of glucuronic acid. The new reagent is advantageous over the usual naphthoresorcinol in the stability on storage, both in crystalline and solution state, and it exhibits higher absorbancy and better reproducibility. The standard procedure was established. It has been found that the measurement of glucuronide with this reagent in the presence of glucuronic acid is possible by employing an alkaline bromine method instead of hypoiodide procedure described by Fishman, et al.

Studies on the Microanalysis of Essential Oil Components. V. Detection of Essential Oil Components by Paper Electrophoresis.

林敬一郎

公開日: 2008年02月19日

P518-524

Extensive studies were made for the detection of terpene alcohols, aldehydes, ketones, and lactones by paper electrophoresis. The method is generally available for a rapid test of perfume products and it could be accomplished more rapidly than chromatography on paper by using a current of 500∼8, 000 V, reported previously. The higher the voltage, the sooner the results are obtained in electrophoresis, while a constant time was required in chromatography owing to the constant capillarity of the filter paper itself. One of many electrolytes applied, mercuric chloride, has shown the most satisfactory result and a formation of conjugated carbonyl groups with mercuric ion was presumed.

Bromination of Cyclic 1, 3-Diketone Monoenolates with N-Bromosuccinimide. I.

荒川基一, 入江昌親

公開日: 2008年02月19日

P524-527

The position of bromine substituted by bromination of 1, 3-cyclohexanedione monoenolate with N-bromosuccinimide was investigated. 1, 3-Cyclohexanedione monoenolates, which have no or one aryl substituent in their 5-position, were found to be brominated with the N-bromosuccinimide at the 2-position.

Bromination of Cyclic 1, 3-Diketone Monoenolates with N-Bromosuccinimide. II.

荒川基一

公開日: 2008年02月19日

P528-531

The position of the substituted bromine in bromination of 1, 3-cyclohexanedione monoenolate with N-bromosuccinimide was investigated. 1, 3-Cyclohexanedione-3-monoenolates, which have two alkyl substituents at their 5-position, were found to be brominated at positions other than 2. From the data obtained in infrared spectra, the stereochemical situations of the bromo substitution were discussed. In this reaction dibromo compounds were obtained as by-products which were not found in a similar reaction for 1, 3-cyclohexanedione monoenolates having no or one aryl substituent at their 5-positions.

Bromination of Cyclic 1, 3-Diketone Monoenolates with N-Bromosuccinimide. III.

荒川基一

公開日: 2008年02月19日

P531-534

The position of substituted bromine in the product obtained by bromination with N-bromosuccinimide of 1, 3-cyclohexanedione 3-monoenolates having two alkyl substituents at the 5-position was established as 6, probably in axial conformation.

Antibacterial Activity of Compounds possessing a Tricarbonylmethane Group. XI. Synthesis of a Compound having Structure analogous to A-Ring of Tetracycline.

浮田忠之進, 荒川基一

公開日: 2008年02月19日

P535-538

Two synthetic routes to a compound having the structure analogous to the A-ring of tetracycline, 2-phenylcarbamoyl-5, 5-dimethyl-6-(1-piperidyl)-1, 3-cyclohexanedione, were established. The desired compound was obtained by amination of 2-phenylcarbamoyl-5, 5-dimethyl-6-bromo-1, 3-cyclohexanedione with piperidine. The antibacterial properties of the final product are reported.

Antibacterial Effect of Lichen Substances and Related Compounds. V. Dibenzofuran Derivatives. (3).

名取信策

公開日: 2008年02月19日

P539-547

About sixty kinds of dibenzofuran derivatives having one or two substituents were synthesized, and relationship between kinds and positions of substituents and antibacterial action, especially against Mycobac. tuberc. A. T. C. C. No. 607, was discussed.

Antibacterial Effect of Lichen Substances and Related Compounds. VI. Dibenzothiophene, Fluorene, and Carbazole Derivatives.

名取信策, 伊藤昌男, 中込孟也

公開日: 2008年02月19日

P548-552

About forty kinds of dibenzothiophene, fluorene, and carbazole derivatives were synthesized and the relationship between chemical structure and antibacterial action, especially against Mycobac. tuberc. A. T. C. C. No. 607, was elucidated in comparison with these of dibenzofuran derivatives.

Antibacterial Effect of Lichen Substances and Related Compounds. VII. The Structure-Activity Relationship observed in Compounds related to Dibenzofuran and an Approach to the Elucidation of the Mode of Action.

名取信策

公開日: 2008年02月19日

P553-560

The relationship between the chemical structure and antibacterial activity observed in compounds related to dibenzofuran was conclusively elucidated. Some attempts were also made for studying the mode of action of these compounds.

Metabolism of Drugs. XIII. The Metabolic Fate of Methylhexabital (5-Cyclohexenyl-3, 5-dimethylbarbituric Acid). (5). Further Studies on Isolation, Characterisation, and Identification of Biotransformation Products of the Drug excreted in the Urine of Rabbit.

吉村英敏

公開日: 2008年02月19日

P561-564

Additional three metabolites of methylhexabital (MHB, 5-cyclohexenyl-3, 5-dimethylbarbituric acid) were isolated from the urine of rabbits receiving MHB and chemical structures of two of these compounds were established as 5-(3-oxo-1-cyclo-hexenyl)-5-methylbarbituric acid and β-5-(3-hydroxy-1-cyclohexenyl)-3, 5-dimethyl-barbituric acid. The main metabolites obtained to date were diastereoisomeric 3-OH-MHB[α-and β-5-(3-hydroxy-1-cyclohexenyl)-3, 5-dimethylbarbituric acid, in which α-form was considerably predominant]and 3-keto-MHB[5-(3-oxo-1-cyclohexenyl)-3, 5-dimethyl-barbituric acid].

Metabolism of Drugs. XIV. Metabolic Fate of p-Aminosalicylic Acid in the Rabbit. (2)

塚元久雄, 山本陽, 鎌田理

公開日: 2008年02月19日

P565-569

The ester-type PAS-glucuronide was isolated from the urine of rabbit receiving PAS and the structure was established as methyl (4-acetamido-2-acetoxybenzoyl 2, 3, 4-tri-O-acetyl-β-D-glucopyranosid) uronate, which was synthesized. m-Aminophenyl glucuronide was isolated from the urine of rabbit. p-Aminosalicyluric acid, m-aminophenyl sulfate, and the ether-type PAS-glucuronide were detected in the urine by means of paper chromatography.

Metabolism of Drugs. XV. Isolation and Paper Chromatography of Urinary Glucuronide of Salicylic Acid in the Rabbit.

塚元久雄, 加藤敬太郎, 辰己淳

公開日: 2008年02月19日

P570-572

Both ether and ester glucuronides of salicylic acid were detected by paper chromatography in the urine of rabbits receiving salicylic acid. The ether glucuronide was isolated as methyl (o-methoxycarbonylphenyl 2, 3, 4-tri-O-acetyl-β-D-glucopyranosid) uronate and the structure was confirmed with the synthetic compound.

Metabolic Products of Fungi. XIII. The Structure of Oxyskyrin.

柴田承二, 滝戸道夫, 太田明広, 黒須玉

公開日: 2008年02月19日

P573-575

The pigment B, isolated from Penicillium islandicum SOPP, N. R. R. L. 1175, and also found in the mycelium of Endothia parasitica ANDERSON ET ANDERSON, was studied. The pigment B which was named oxyskyrin gave a molecular formula, C₃₀H₁₈O₁₁, and yielded heptaacetate and heptabenzoate. On reductive cleavage with alkaline sodium dithionite, oxyskyrin was decomposed to give emodin and ω-hydroxyemodin. On oxidation with chromium trioxide, oxyskyrin heptaacetate was converted into skyric acid hexaacetate. Consequently, oxyskyrin was formulated as 2, 4, 5, 2', 4', 5'-hexahydroxy-7-methyl-7'-hydroxymethyl-bianthraquinone-(1, 1').

The Use of Radioactive Element. II. Decomposition of 1, 4-Dibenzoyl-thiosemicarbazide and 1, 4-Dibenzoylsemicarbazide with Alkali.

中井利三郎, 杉井通泰, 中尾英雄

公開日: 2008年02月19日

P576-579

1, 4-Dibenzoylthiosemicarbazide (II) is converted by the action of alkali principally into 3-phenyl-5-mercapto-1, 2, 4-triazole (IV) and benzoic acid. The reaction route was studied by using ¹⁴C-tracer technique. It was thereby found that (II) affords 1-benzoyl-thiosemicarbazide (A) and benzoic acid in the first step and (A) further cyclizes to (IV), while a part of (A) decomposes into benzoic acid and ammonia. 1, 4-Dibenzoylsemicarbazide also behaves in analogous manner.

Chemicopharmacological Studies on Antispasmodic Action. IX. Precise Discrimination of Atropine-like Activity and Papaverine-like Activity as Competitive and Non-competitive Antagonism to Acetylcholine.

高木敬次郎, 高柳一成

公開日: 2008年02月19日

P580-587

(1) ACh dose-response curve in the presence of various concentrations of antagonist was traced fully and it was suggested experimentaly that the curve moved parallel by the atropine-like action and its maximum response was depressed noncompetitively by the papaverine-like action. (2) It was made possible to discriminate precisely the atropine-like action as competitive antagonism to a low concentration of ACh 4×10^-8g./cc. and the papaverinelike action as non-competitive antagonism to a high concentration of ACh (1.11×10^-4g./cc.). (3) The potency ratios in relaxing the contraction due to the high concentration of ACh was almost the same as the ratios against BaCl₂.

4, 5-Substituted Pyridazines. III. Oxidation and Solvolysis of 4-Methyl-3, 6-dichloropyridazine.

倉石典

公開日: 2008年02月19日

P587-589

1) 4-Methyl-6-chloro-3-pyridazinol (IIIa) and 5-methyl-6-chloro-3-pyridazinol (IIIb) were obtained from 4-methyl-3, 6-dichloropyridazine (I) by refluxing with glacial acetic acid. 2) 4-Carboxy-6-chloro-3-pyridazinol (II) was formed from 4-methyl-3, 6-dichloropyridazine (I) and 4-methyl-6-chloro-3-pyridazinol (IIIa) by oxidation with potassium dichromate in conc. sulfuric acid and it was led to ester (VI), hydrazide (VII), and amide (VIII) derivatives. 3) 5-Carboxy-6-chloro-3-pyridazinol (IX) was also obtained by similar procedure from 5-methyl-6-chloro-3-pyridazinol (IIIb).

Microanalysis of Amino Acids. II. On the Amino Acid Content of Beet Molasses from Hokkaido.

塚本赳夫, 古森徹哉, 木下洋夫

公開日: 2008年02月19日

P590-594

Nineteen kinds of amino acid contained in beet molasses from Hokkaido were quantitatively separated and analyzed by the new method in which ion exchanger and paper partition chromatography were applied, when the amino acids were mixed with sugars, proteins and other inorganic substances.

Phytochemical Investigation on Cultivation of Medicinal Plants. XIV. On the Alkaloid Biogenesis in Ephedra. (4).

柴田承二, 今関和泉, 山崎幹夫

公開日: 2008年02月19日

P594-597

It was proved that formate labeled with ¹⁴C is incorporated into γ-methyl and Nmethyl groups in l-ephedrine molecule in Ephedra distachya. The mechanism of biosynthesis of ephedrine coupling with the C₁-fragment incorporation is discussed.

Application of Chromatography. XXXIII. V-Compound Isolated from the Mycelium of Eremothecium ashbyii.

増田亨, 貴志豊和, 浅井満子

公開日: 2008年02月19日

P598-606

The purple fluorescent substance (V-compound) obtained by the authors from the mycelium of Er. ashbyii occurs as colorless needles, m. p. 263°(decomp.), [α]²⁰_D : +4.5°(in H_2O), +11.45°(in 0.1N NaOH). The molecular weight of this substance was found to be about 300 by Barger method, titration (as monobasic acid), and from the wave height in polarography. A molecular formula of C₁₂H₁₆O₇N₄ was assigned to the substance from its analytical value. From its ultraviolet and infrared spectra the presence of a pteridine ring, COOH, and OH was presumed. Since the substance gave urea by treatment with alkali solution, it was assumed to be a pteridine compound having a carbonyl group at 2-position, substituted by a group at one of the nitrogens in the pyrazine ring. From the fact that the acetylation product of the substance was in accord with its tetraacetate, and that it gave formaldehyde by oxidation with lead tetraacetate, the group was presumed to be ribityl. Photodecomposition of this substance furnished more important data. Although exposure of an aqueous solution of the substance to direct sunlight destroyed even the pteridine ring, irradiation of its alkaline solution with light from an electric lamp in the presence of hydrogen peroxide yielded crystals of m. p. >360°. The product exhibited the ultraviolet spectrum characteristic to pteridine compounds. Comparison of the product with lumazine-6-carboxylic acid by ionophoresis indicated that the former has lower negative charge than the latter. Therefore, the molecular formula, C₇H₆O₄N₄, calculated from the analytical value was concluded to be C₇H₄O₃N₄·H₂O. This may be due to the dehydrogenation of the parent ring during cleavage of the group at the nitrogen of the pyrazine ring by photodecomposition of the V-compound. From these results, the authors gave the following structure to the V-compound.

Polarisation der heterocyklischen Ringe mit aromatischem Charakter. CXX. Eine neue Synthese von 1-Halogeno-5, 6, 7, 8-tetrahydroisochinolin.

落合英二, 川添豊

公開日: 2008年02月19日

P606-610

Durch katalytische Reduktion von 1-Aminoisochinolin mit PtO₂ in Eisessig-Losung wurde 1-Amino-5, 6, 7, 8-tetrahydroisochinolin in 70%iger Ausbeute erhalten. Das letztere wurde nach Grewe in 1-Brom-5, 6, 7, 8-tetrahydroisochinolin mit einer Ausbeute von 71% ubergefuhrt. 1-Amino-5, 6, 7, 8-tetrahydroisochinolin gab beim Diazotieren 5, 6, 7, 8-Tetrahydroisocarbostyril in einer Ausbeute von 90%, welches auch durch direkte Reduktion von Isocarbostyril in einer Ausbeute von 40% erhalten wurde. 5, 6, 7, 8-Tetrahydroisocarbostyril gab beim Erhitzen mit Phosphoroxychlorid 1-Chlor-5, 6, 7, 8-tetrahydroisochinolin mit einer Ausbeute von 80%.

Studies on the Microanalysis of Essential Oil Components. IV. The Spot Test of Essential Oil Components by Antimony Pentachloride.

林敬一郎, 橋本庸平

公開日: 2008年02月19日

P611-613

Amongst numerous color tests for essential oil components present, 10% chloroform or ethylene dichloride with 0.01% iodine solution of antimony pentachloride was regarded to be most excellent so far as the instantaneous spot test was concerned. The majority of compounds belonging to the category of essential oil constituents produced characteristic colors by merely touching the reagent to the sample on filter paper, without any additional treatment.

Effect of Biogenic Amines on Yeast Carboxylase.

林誠, 山脇豊, 宮木高明

公開日: 2008年02月19日

P614

本文PDF[265K]

Formamidinesulfinic Acid as a Reducing Agent. I.

高木誠司, 田中久, 横山陽

公開日: 2008年02月19日

P615-616

本文PDF[331K]

Synthesis of Indolil Aryl 1, 2-Diketones

高木誠司, 杉井篤, 町田勝之輔

公開日: 2008年02月19日

P617-618

本文PDF[370K]

Notiz uber einige neue Diphenylather-aldehyde und deren Thiosemicarbazone.

伊藤源蔵, 柴沼由久

公開日: 2008年02月19日

P619-621

4'-Hydroxy-4-formyl-, 4'-Carboxy-4-formyl- und 4, 4'-Diformyldiphenylather wurden aus den entsprechenden Methyldiphenylathern uber Bromverbindungen synthetisiert und deren Thiosemicarbazone dargestellt.

Uber ein phenolisches Nebenprodukt bei der Darstellung von Lepidin-N-oxyd.

落合英二, 谷田博

公開日: 2008年02月19日

P621-622

本文PDF[333K]

The Conversion of Alantolactone into Dihydroeudesmol

田辺克巳

公開日: 2008年02月19日

P623-624

本文PDF[324K]

Detection of Hydroxyl Derivatives from the Urine of Men administered Ethylhexabital and Methylhexabital by Buffered Paper Chromatography.

塚元久雄, 土岐智, 金田旭立

公開日: 2008年02月19日

P625-626

本文PDF[344K]

Studies on Digitalis Glycoside. Acetyldigitoxin-α from Digitoxin.

佐藤大助, 尾山蓉子, 奥村保

公開日: 2008年02月19日

P627

本文PDF[252K]

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後続誌

巻号一覧
Pharmaceutical Bulletin

Pharmaceutical Bulletin Vol. 5(1957) No. 6

Biochemical Studies on Pathogenic Fungi. VI. Nutritional Studies on Trichophyton gypseum with Special Reference to its Pleomorphism.

Biochemical Studies on Pathogenic Fungi. VII. The Effect of Synthetic Fungicides and Fatty Acids on the Respiration of Trichophyton gypseum.

Biochemical Studies on Pathogenic Fungi. VIII. The Effect of an Antibiotic, Trichomycin, on the Respiration and Phosphorus Metabolism of Trichophyton gypseum.

Naphthoresorcinol Picrate for the Determination of Glucuronic Acid in Physiological Materials.

Studies on the Microanalysis of Essential Oil Components. V. Detection of Essential Oil Components by Paper Electrophoresis.

Bromination of Cyclic 1, 3-Diketone Monoenolates with N-Bromosuccinimide. I.

Bromination of Cyclic 1, 3-Diketone Monoenolates with N-Bromosuccinimide. II.

Bromination of Cyclic 1, 3-Diketone Monoenolates with N-Bromosuccinimide. III.

Antibacterial Activity of Compounds possessing a Tricarbonylmethane Group. XI. Synthesis of a Compound having Structure analogous to A-Ring of Tetracycline.

Antibacterial Effect of Lichen Substances and Related Compounds. V. Dibenzofuran Derivatives. (3).

Antibacterial Effect of Lichen Substances and Related Compounds. VI. Dibenzothiophene, Fluorene, and Carbazole Derivatives.

Antibacterial Effect of Lichen Substances and Related Compounds. VII. The Structure-Activity Relationship observed in Compounds related to Dibenzofuran and an Approach to the Elucidation of the Mode of Action.

Metabolism of Drugs. XIII. The Metabolic Fate of Methylhexabital (5-Cyclohexenyl-3, 5-dimethylbarbituric Acid). (5). Further Studies on Isolation, Characterisation, and Identification of Biotransformation Products of the Drug excreted in the Urine of Rabbit.

Metabolism of Drugs. XIV. Metabolic Fate of p-Aminosalicylic Acid in the Rabbit. (2)

Metabolism of Drugs. XV. Isolation and Paper Chromatography of Urinary Glucuronide of Salicylic Acid in the Rabbit.

Metabolic Products of Fungi. XIII. The Structure of Oxyskyrin.

The Use of Radioactive Element. II. Decomposition of 1, 4-Dibenzoyl-thiosemicarbazide and 1, 4-Dibenzoylsemicarbazide with Alkali.

Chemicopharmacological Studies on Antispasmodic Action. IX. Precise Discrimination of Atropine-like Activity and Papaverine-like Activity as Competitive and Non-competitive Antagonism to Acetylcholine.

4, 5-Substituted Pyridazines. III. Oxidation and Solvolysis of 4-Methyl-3, 6-dichloropyridazine.

Microanalysis of Amino Acids. II. On the Amino Acid Content of Beet Molasses from Hokkaido.

Phytochemical Investigation on Cultivation of Medicinal Plants. XIV. On the Alkaloid Biogenesis in Ephedra. (4).

Application of Chromatography. XXXIII. V-Compound Isolated from the Mycelium of Eremothecium ashbyii.

Polarisation der heterocyklischen Ringe mit aromatischem Charakter. CXX. Eine neue Synthese von 1-Halogeno-5, 6, 7, 8-tetrahydroisochinolin.

Studies on the Microanalysis of Essential Oil Components. IV. The Spot Test of Essential Oil Components by Antimony Pentachloride.

Effect of Biogenic Amines on Yeast Carboxylase.

Formamidinesulfinic Acid as a Reducing Agent. I.

Synthesis of Indolil Aryl 1, 2-Diketones

Notiz uber einige neue Diphenylather-aldehyde und deren Thiosemicarbazone.

Uber ein phenolisches Nebenprodukt bei der Darstellung von Lepidin-N-oxyd.

The Conversion of Alantolactone into Dihydroeudesmol

Detection of Hydroxyl Derivatives from the Urine of Men administered Ethylhexabital and Methylhexabital by Buffered Paper Chromatography.

Studies on Digitalis Glycoside. Acetyldigitoxin-α from Digitoxin.

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Pharmaceutical Bulletin Vol. 5(1957) No. 6

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巻号一覧
Pharmaceutical Bulletin