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武久 善孝, 川副 裕一, 田口 胤三
1976 年 24 巻 8 号 p.
1691-1697
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The reaction of anti-oxime (1) of 2-phenoxycyclohexanone was attempted in continuation of the former studies on the Grignard reactions of oximes. Consequently, it ended in a result entirely different from the Hoch-Campbell reaction and also the intramolecular ringclosure reaction which has been previously reported. causing the elimination of phenol and the productions of aniline and 2-phenoxycyclohexanone in main. The reaction pathway was discussed. Additionally, the government of reaction by both changes of 2-substituent on cyclohexanone oxime and Grignard reagent was preliminarily examined.
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杉浦 衛, 平野 和行, 飯野 四郎, 鈴木 宏, 織田 敏次
1976 年 24 巻 8 号 p.
1698-1703
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Alkaline phosphatase (E. C. 3. 1. 3. 1) from human kidney was purified by n-butanol extraction, ammonium sulfate fractionation, and chromatography over DEAE-cellulose, CM-cellulose, and Sephadex G-200. The purified enzyme exhibited a single protein band by disc electrophoresis. This enzyme was activated by MgCl
2 and NiCl
2, but inhibited by CdCl
2, and had an optimum pH at 11.4. Other properties of kidney alkaline phosphatase were also investigated and discussed.
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小林 義郎, 熊懐 稜丸, 浜名 洋
1976 年 24 巻 8 号 p.
1704-1707
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Alkylation of 1-position of 5-methyl-1, 2, 3, 4-tetrahydro-1, 6-naphthyridine (I) does not proceed in ordinary methods. I shows quite peculiar behavior in ultraviolet spectrum ; absorption maximum shows bathochromic shift on protonation. Based on these data alkylation was successfully carried out in the presence of sodium amide.
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古川 潮, 須田 千秋, 林 清五郎
1976 年 24 巻 8 号 p.
1708-1713
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
New compounds of N-(substituted thio) isatins (III) were synthesized and reactions with several nucleophiles were examined in comparison with the reaction using N-(substituted thio) phthalimides (I) and N-(substituted thio) succinimides (II) : All of I, II, and III reacted with organometallic compounds, cyanide ion, and trichloromethyl carbanion to give sulfides (IV), thiocyanates (V), and trichloromethyl sulfides (VI) respectively. Different from I and II, however, the reaction of III with amines afforded 3-amino-1-substituted thio-3-hydroxy-2-oxo-indoles (X), with no formation of any sulfenamides anticipated.
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吉田 誠一郎, 釜野 徳明, 酒井 健
1976 年 24 巻 8 号 p.
1714-1717
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The surface anesthetic activities of ten bufadienolides, i. e., resibufogenin, bufalin, bufotalin, desacetyl-bufotalin, cinobufagin, desacetyl-cinobufagin, cinobufotalin, desacetyl-cinobufotalin, telocinobufagin and marinobufagin, were studied using the guinea pig cornea. With exceptions of resibufogenin and marinobufagin, all substances tested were more effective than cocaine. Their anesthetic activities were in the following order : bufalin > telocinobufagin > bufotalin > cinobufagin > cinobufotalin > desacetyl-bufotalin ≨ desacetyl-cinobufagin ≨ desacetyl-cinobufotalin. Resibufogenin and marinobufagin had no appreciable effect on the cornea. There is some correlation between the chemical structure and the surface anesthetic activity in the bufadienolides tested.
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宮崎 利夫, 直井 家寿太
1976 年 24 巻 8 号 p.
1718-1723
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Major water-soluble polysaccharide obtained from the cell wall of Cladosporium trichoides by diethylaminoethyl-cellulose column fractionation is a heteroglycan, [α]
20
D+50°(c=1, H
2O), which is composed of D-galactose, D-glucose, D-mannose, and small amount of L-rhamnose (1.4 : 1.4 : 1.0 : 1.0). The results of periodate oxidation, Smith-type degradation, methylation, and gas-liquid chromatography-mass spectrometry spectra show that the polysaccharide has branched structure and contains 1, 2-, and 1, 2, 6-linked galacto-furanosyl, 1, 3, 6-linked mannopyranosyl, and a small amount of 1, 4-linked glucopyranosyl residues as the main units. The terminal residues are glucopyranosyl and mannopyranosyl residues.
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萩下 山治, 栗山 馨
1976 年 24 巻 8 号 p.
1724-1730
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
threo-1-Hydroxy-2-(isopropylamino)-[10]-paracyclophane (1) was prepared and resolved into one enantiomer. The absolute configuration of 1 was deduced from the analysis of circular dichroism (CD) spectra using Snatzke's sector rule and induced CD of Cu(su)
2(ip)
2 and Pr(DPM)
3. Intrinsic sympathomimetic activity of 1 and threo-and erythro-1-(4-tolyl)-2-isopropylamino-1-propanol were tested on the isolated guinea pig heart.
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秋葉 光雄, 小杉 義幸, 高田 豊造
1976 年 24 巻 8 号 p.
1731-1736
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Indazoloquinone (4) or 5-substituted indazoloquinones (5a-c) were obtained with an acid-catalyzed substitution reaction of mono-(2a-c) or diaminoquinone tosylhydrazones (3a-c) in high yields. The reaction mechanism and rate were investigated.
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本橋 範子, 森 五彦, 杉浦 幸雄
1976 年 24 巻 8 号 p.
1737-1741
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
^13C-Nuclear magnetic resonance (CMR) and Raman spectra of ergothioneine and its mercury complex have been recorded as function of pH. The
13C-signals of ergothioneine is assigned by comparison with the chemical shifts of histidine, 2-mercaptoimidazole and betaine. Ergothioneine is present in thione form in an aqueous solution or a solid state. In basic solution, ergothioneine exists as thiolate ion upon the deprotonation of the imidazole ring, and the tautomeric form of its imidazole ring is predominantly the 1-H tautomer. The result of
13C-NMR and raman spectra support that ergothioneine coordinates to Hg (II) ion through the thiolate sulfur.
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木付 和幸, 森脇 千秋, 法島 義男, 守屋 寛
1976 年 24 巻 8 号 p.
1742-1748
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Potent kininase activities were found in Japanese mushrooms. Especially Tricholoma conglobatum (shimeji, in Japanese) contained 40-334 kininase units/g and the enzyme was purified by water extraction, ammonium sulfate fractionation, diethylaminoethyl (DEAE)-Sephadex A-50 chromatography and Sephadex G-100 gel filtration. The final preparation gave a single band in disc electrophoresis and its kininase activity, that was expressed in terms of μg bradykinin degraded in 1 min at 30°, was 480 units/E
280. This value was extremely potent, so this enzyme could be expected as a useful agent on the clinical purposes or other investigations of kallikrein-kinin system. The sites of action of this enzyme on bradykinin molecule were investigated by examination of 1-dimethylaminonaphthalene-5-sulphonyl (DNS)-modified products, which were liberated from bradykinin by this enzyme, on thin layer chromatography. It cleaved Gly
4-Phe
5 and Pro
7-Phe
8 bonds and the former bond was split more easily than the latter one.
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中川 彰, 鈴木 数広, 岩崎 克義, 梶 清文, 大村 智, / , MAX TISHLER
1976 年 24 巻 8 号 p.
1749-1756
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
An aglycone moiety of leucomycin-A
3 (1), leuconolide-A
3-5, 18-hemiacetal (3), was isolated by the application of a modified Polonovski-reaction to leucomycin-A
3 N-oxide (2). Two neutral macrolides, 2'-O-acetyl-3'-N-desdimethylamino-3'-oxo-leucomycin-A
3 (5) and 2'-O-acetyl-3'-N-desmethyl-N-acetyl leucomycin-A
3 (8) in which the mycaminose moiety of 1 was modified, were also isolated from the same reaction. In a similar manner, an aglycone, 9-dehydro-18-dihydro-leuconolide-A
3 (12) was obtained from 9-dehydro-18-dihydro-leucomycin-A
3 (10). While the latter as an isomer of 1, differing with respect to the position of carbonyl group on the lactone ring, has significant antimicrobial activity neither its aglycone 12 nor the aglycone of leucomycin-A
3 show antimicrobial activity.
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橋本 進一郎, 志津 三千代, 高橋 史郎
1976 年 24 巻 8 号 p.
1757-1764
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The in vitro metabolism of generally labelled
3H-3-(1-hydroxy-2-piperidinoethyl)-5-phenylisoxazole (
3H-31252-S) using the 9000xg supernatant fraction of rabbit liver homogenate was studied. The metabolites were indentified and determined quantitatively by reverse isotope dilution analysis. The results indicated that it was extensively metabolized and the main metabolic pathways were N-oxidation of piperidine and p-hydroxylation of phenyl ring. 3-{1-Hydroxy-2-(4-hydroxypiperidino) ethyl}-5-phenylisoxazole (XVII) showed slightly stronger analgesic activity than the parent compound 31252-S. All metabolites were less foxic than the parent 31252-S.
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大石 秀夫, 牛尾 洋一, 栖原 和美, 竹原 光教
1976 年 24 巻 8 号 p.
1765-1773
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Comparative studies of oily vehicles, hydrocarbons (HC), esters (E), and tri-glycerides (TG), were done on percutaneous absorption of salicylic acid (SA), physicochemical parameters. and trans-epidermal water loss(TEWL) in rat. The diffusion concept was supported experimentally ; vehicle viscosity was found to be an important restriction factor of drug absorption. In HC, which had low affinity to SA as estimated by solubility and partition coefficient, good correlation was obtained between drug absorption and viscotity, but this correlation could be seen only within the series. In spite of using the same series, the reverse effect was obtained in the lower molecular weight range of TG ; absorption decreased according to increase in affinity to SA, and maximum absorption appeared with the medium-chain length TG. In E, the skin-altering effect may have a rather important role in absorption, although the viscosity effect was seen. TEWL was suppressed by HC, promoted by E. and promoted slightly by TG. TEWL values correlated well with SA absorption suggesting the importance of the physiological effect of the vehicle in drug absorption.
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中川 俊夫, 竹原 光教, 大石 秀夫
1976 年 24 巻 8 号 p.
1774-1778
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Drug absorption across the skin has been interpreted as the diffusional mass transfer of the drug starting from the vehicle, travelling through the skin tissue, and terminating at the blood stream. There may be some non-diffusional resistance against the drug migration at the vehicle-skin interface and the skin-blood interface. Simulation calculation using an electronic computer can be applied to this simple model of the thickness of the administrated vehicle, that of the skin, the diffusion coefficient in the vehicle, that in the skin, the partition coefficient between these two phases, and the non-diffusional resistance at the vehicle-skin and the skin-blood interface. The present paper describes the method of simulation which has been applied to the experimental results detailed in the succeeding paper.
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竹原 光教, 中川 俊夫, 牛尾 洋一, 栖原 和美, 大石 秀夫
1976 年 24 巻 8 号 p.
1779-1783
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Diffusion coefficients of salicylic acid (SA) in the vehicles and the skin and partition coefficients of SA between the intact or stripped skin and a saline solution were measured, the simulation of drug absorption from the vehicles, based on the theory in Part II, was carried out, and the proportionalities between the calculated and the experimental absorption values were sufficient for all vehicles. It was found that the skin layer has an unknown nondiffusional resistance by an absorption experiment through the stripped skin. Volume effect of the drug phase on the percent absorption was interpreted by an accumulation of the vehicle at the circumference of the cell caused by an interfacial tension between the vehicle and the cell.
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原田 正敏, 藤井 祐一, 神谷 譲二
1976 年 24 巻 8 号 p.
1784-1788
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Effects of cinnamaldehyde (CA), the main component of Chinese cinnamon which has frequently been prescribed as a remedy in Chinese medicine, on the spontaneous electroencephalograms (EEGs) as well as on the recruiting response and the augmenting response in rabbits were studied. CA converted resting patterns in the EEGs recorded from the frontal cortex, the hippocampus, the amygdala, and the midbrain reticular formation to arousal patterns in the gallamine-paralyzed preparation with the intact brain. In the midpontine pretrigeminal transected preparation, CA also induced an arousal pattern in the electrocorticogram (ECoG). In the low cerveau isole preparation, CA either converted a resting pattern in the ECoG to a sequence of low voltage fast waves or did not elicit such an action depending upon each individual preparation. In the high cerveau isole preparation, CA was not capable of producing any effect on the ECoG. CA, in higher doses, inhibited the recruiting response and the augmenting response. It was concluded that CA produced a centrally originating EEG activation through a direct or indirect excitatory action on the brainstem reticular formation.
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北森 信之, 島本 次雄
1976 年 24 巻 8 号 p.
1789-1794
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
A study was made on the effect of dimensions on the disintegration time of tablet. The ln-ln plot of the disintegration time against the tablet thickness gave a straight line. The relation may be expressed simply by the equation, t
D=KT
n where t
D is the disintegration time of the tablet which is compressed at a fixed pressure and has a constant diameter and thickness T, and K and n are constants. The relation expressed by this equation held good not only for directly compressed tablets but also for tablets made from granules. A tablet disintegration mechanism can be assumed by this equation. The rate of deaggregation of particles from the surface of the tablet changes with time depending upon the degree of the acceleration of deaggregation through the swelling of the disintegrant.
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恩田 政行, 矢吹 玲子, 竹内 啓二, 根田 八重子
1976 年 24 巻 8 号 p.
1795-1798
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The compounds obtained from alumina-induced reaction of 3β, 5α-diacetoxy-6-nitri-minocholestane (3) are revised as 3β-acetoxy-6-Nα-, 7α-(4) and 7β-O-(Nβ-oxido) diazoxy-cholest-5-ene (5) the basis of their spectral data. Formation pathways of the oxadiazoles (4) and (5) from the nitrimine (3) and conversion pathways of the oxadiazoles (4) and (5) into 3β-acetoxy-6-formyl-B-nor-cholest-5-ene (8) are briefly examined.
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森口 郁生, 叶田 やよい, 小松 克一郎
1976 年 24 巻 8 号 p.
1799-1806
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The correlations of Hansch's hydrophobic constant (log P) with van der Waals volume (Vw) and with van der Waals surface area (Aw) were studied using 60 molecules including apolar organic compounds and inert gases, and superiority of Vw over Aw was recognized. From the obtained highly significant relation of Vw to log P and a great number of log P values for polar molecules, hydrophilic effects (Vw) of various polar groups were evaluated. These parameters (Vw and Vw) could be satisfactorily applied to the regression analysis of water-solubility of 156 organic liquids and frog muscle narcosis of 39 drugs. These parameters may especially be useful for drug design because they can easily be calculated for a wide variety of molecules.
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友田 正司, 木村 里美
1976 年 24 巻 8 号 p.
1807-1812
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Partial acetolysis of Bletilla-glucomannan, the mucilage from the tubers of Bletilla striata REICHENBACH fil., has led to the isolations of fourteen oligosaccharides. Analysis of components, methylation and partial degradation studies provided the evidences that they are O-β-D-mannopyranosyl-(1→4)-D-mannopyranose, O-α-D-mannopyranosyl-(1→4)-D-mannopyranose, O-β-D-mannopyranosyl-(1→4)-D-glucopyranose, O-β-D-glucopyranosyl-(1→4)-D-mannopyranose, O-β-D-glucopyranosyl-(1→4)-D-glucopyranose, O-β-D-mannopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-mannopyranose, O-β-D-glucopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-mannopyranose, O-β-D-mannopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-glucopyranose, O-β-D-mannopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-glucopyranose, O-β-D-mannopyranosyl-(1→4)-O-β-D-glucopyranosyl-(1→4)-D-mannopyranose, O-β-D-glucopyranosyl-O-β-D-glucopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-mannopyranose, O-β-D-mannopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-mannopyranose, O-β-D-glucopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-mannopyranose, and O-β-D-mannopyranosyl-(1→4)-O-β-D-glucopyranosyl-(1→4)-O-β-D-mannopyranosyl-(1→4)-D-mannopyranose. Among them, it is conceivable that mannobiose having α-glycosidic linkage is the artifact produced during the reaction.
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竹内 烈, 濱田 喜樹
1976 年 24 巻 8 号 p.
1813-1821
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
1, 7-Naphthyridine (II) was prepared by the reduction of 8-chloro-1, 7-naphthyridine over palladium-carbon. 1, 5-Naphthyridine 1-oxide (III) and 1, 5-naphthyridine (IV) were synthesized by the reaction of 3-aminopyridine 1-oxide with glycerol in the presence of Sulfo-mix, ferrous sulfate, and boric acid. Phenylation of 1, X-naphthyridine (X=5, 6, 7, and 8) with phenyllithium afforded monophenylated compounds, phenyllithium having reacted in the 2-position. Methylation of II with methylsulfinyl carbanion afforded 4, 8-dimethyl-1, 7-naphthyridine (XI), and the Reissert reaction of II with benzoyl chloride and potassium cyanide afforded the normal Reissert compound (XII). Insecticidal activity of V, VIII-X, and XIII-XVIII was also examined.
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杉浦 衛, 磯部 正和
1976 年 24 巻 8 号 p.
1822-1828
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The hydrolytic activity of the lipase (EC 3. 1. 1. 3) from Chromobacterium for the monomeric esters was found. The hydrolysis of p-nitrophenyl acetate by the lipase proceeded with three step reaction in which acylation and deacylation processes of the enzyme were involved. The rate limiting step was found to be the acylation. The enzymic hydrolysis was accelerated about 2-fold by the additions of hydrophobic glass beads. Water soluble organic solvents did not activate but inhibit the enzymic hydrolysis and they did not affect significantly on the activating effect by hydrophobic glass beads. It was found that the lipase was adsorbed on the glass beads and once adsorbed enzyme was difficult to desorb. These results were discussed relation to the reaction mechanism of lipolysis by lipase and an assumption was made.
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恩田 政行, 竹内 啓二
1976 年 24 巻 8 号 p.
1829-1831
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Photolysis of 3β, 5α-diacetoxy-6-nitriminocholestane (1) gives 3β, 5α-diacetoxycholestan-6-one (2), 3β-acetoxy-5α-cholestan-6-one (8), 3β, 5α-diacetoxy-6-hydroximinocholestane (9), and 3β, 5α-diacetoxy-6-iminocholestane (10) as nitrate. The structure of 10 is proved by its catalytic reduction and subsequent acetylation to 6β-acetamido-3β, 5α-diacetoxycholestane (11). The structure of 9 is identified by its reduction with titanium trichloride to 10. Also, formation pathways of these photo-products are briefly examined.
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宮崎 正三, 中野 真汎, 有田 隆一
1976 年 24 巻 8 号 p.
1832-1838
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
A quantitative method was described which utilized infrared spectroscopy for the determination of chlortetracycline hydrochloride (CTC-HCl) crystalline forms in mixtures. Data were included which demonstrated that the method could be utilized to follow the rate of transformation taking place in the biologically available crystalline form (β form). Transformation of the crystalline form under different conditions such as solid state and aqueous suspension was investigated. The solid CTC-HCl β form was shown to change to the more stable α form in high humidities, over 75% relative humidity (R. H.) at 20°. The rate of transformation was found to be proportional to the humidity. On the other hand, under 65% R. H. no polymorphic transformation was observed for 40 days at 20°. Transformation of the β form was also not detected by heating at 70°. In aqueous suspensions, rapid solution phase transformation was observed from the CTC-HCl β form to the water-stable α form. The rate of transformation in the suspensions was found to be temperature and pH dependent. Results obtained from these transformation studies suggested that water and water vapor were important factors in the transformation of the CTC-HCl β form.
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秋田 安男, 三須 恵子, 渡辺 徳弘, 太田 明広
1976 年 24 巻 8 号 p.
1839-1841
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
N-Oxides of pyridine, quinoline, and pyrazine derivatives were reduced with chromium (II) chloride in acetone, methanol, or chloroform at room temperature to give the deoxygenation products in excellent yields. Quinaldine and 2-ethoxyquinoline 1-oxides, possessing an electron donating group at 2-position of the quinoline ring, were not reduced at room temperature, but, under reflux, the reaction gave the deoxygenation products in good yields. In the case of the reaction of 4-chloroquinoline 1-oxide with chromium (II) chloride for 20 min occured dechlorination and deoxygenation, but for 1 min only deoxygenation. The reaction of 4-nitropyridine 1-oxide and 3-, 4-, and 5-nitroquinoline 1-oxides was not successful.
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坂東 英雄, 山岸 喬, 林 紘司, 三橋 博
1976 年 24 巻 8 号 p.
1842-1844
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
A new 5, 6α-glycolic compound, glycocaudatin, isolated from Cynanchum caudatum, in addition to glycocynanchogenine and 12β-O-cinnamoyl-20-O-acetyl-glycosarcostin, was identical with the derivative obtained in a good yield via the epoxidation of caudatin, which had been isolated from the same plant.
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森 洋樹, 斎藤 恭子, 殿井 靖敏, 熊岡 熙, 赤木 満洲雄
1976 年 24 巻 8 号 p.
1845-1852
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The effect of glucose and galactose on the formation of respiratory enzymes and cytochromes in yeast cells was compared both in aerobic culture and during adaptation of anaerobically grown cells to oxygen. (1) In aerobic culture, activities of reduced nicotinamide-adenine dinucleotide (NADH) cytochrome c reductase and malate dehydrogenase and QO
2 of cells were reduced considerably with increasing concentration of glucose in the medium. On the other hand, galactose did not repress NADH cytochrome c reductase significantly and QO
2 of cells was not reduced with increasing concentration of gllactose in the growth medium, although it slightly repressed malate dehydrogenase. (2) Formation of cytochromes, and NADH cytochrome c reductase and malate dehydrogenase during the adaptation of anaerobic cells to oxygen were inhibited by a high concentration of glucose but not by galactose, and glucose was consumed rapidly but galactose was consumed slowly. On the other hand, when yeast cells grown anaerobically in the presence of galactose were transferred to aerobic culture in the presence of galactose, it was consumed rapidly and the formation of cytochromes, NADH cytochrome c reductase and malate dehydrogenase was inhibited. NADH ferricyanide reductase activity did not changed significantly during the adaptation of anaerobic cells to oxygen.
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山本 譲, 西村 憲一, 桐山 典城
1976 年 24 巻 8 号 p.
1853-1859
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The metabolites of Aspergillus terreus IFO 6123 were studied. 3-Methylorsellinic acid, 4-O-demethylbarbatic acid and a new metabolite named asterriquinone were isolated. The chemical structure of asterriquinone was established as 2, 5-bis-[N-(1", 1"-dimethyl-2"-propenyl)-indoyl-3']-3, 6-dihydroxy-1, 4-benzoquinone by chemical and physical experimental data. The incorporation experiments using
14C-labeled compounds showed that asterriquinone is biosynthesized from tryptophan and isopentenyl unit derived from mevalonate.
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細田 宏, 山下 幸和, 知野 紀子, 南原 利夫
1976 年 24 巻 8 号 p.
1860-1864
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The titled compounds (1, 2) have been prepared from dehydroepiandrosterone. Introduction of the hydroxyl group into the 15α-position was attained by hydroboration of the 14, 15-double bond with diborane and subsequent oxidation of the organoborane with alkaline hydrogen peroxide under the protection of the 5, 6-double bond as the 3, 5-cyclo structure. A simple method for regeneration of the 3β-hydroxy-Δ
5-steroid from the 3, 5-cyclo derivative was also developed.
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浜名 洋, 大倉 洋甫
1976 年 24 巻 8 号 p.
1865-1869
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
A new photometric method is presented for the assay of serum glutamate pyruvate transaminase activity on the basis of the determination of 2-oxoglutaric acid produced in the enzyme reaction under its optimal conditions by means of the previously established method for selective determination of the acid with diazotized sulfamethizole. The method gives reliable results and is simply performed with a small amount of sample with a wide range of activity.
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亀谷 哲治, 木川 良雄, 高橋 多希子, 根本 英雄, 福本 圭一郎
1976 年 24 巻 8 号 p.
1870-1878
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The reaction of 3-carboxy-1, 2-dihydro-1-methyl-2-oxopyridine (V) with diazomethane afforded 6, 7-dihydro-1, 6-dimethyl-7-oxopyrazolo [3, 4-c] pyridine (VI), 4, 5, 6, 7-tetrahydro-1, 6-dimethyl-7-oxopyrazolo [3, 4-c] pyridine (VII), and 1, 2-dihydro-3-methoxycarbonyl-1, 4-dimethyl-2-oxopyridine (VIII). 1-Ethyl-6, 7-dihydro-3, 6-dimethyl-7-oxopyrazolo [3, 4-c] pyridine (XXI), 8a-ethoxycarbonyl-1, 4, 4a, 7, 8, 8a-hexahydro-3, 4, 7-trimethyl-8-oxopyrido [3, 4-c] pyridazine (XXII), and 3-ethoxycarbonyl-4-ethyl-1, 2-dihydro-1-methyl-2-oxopyridine (XXIII) were obtained from the reaction of compound (V) with diazoethane. The treatment of 4-carboxy-1, 2-dihydro-1-methyl-2-oxopyridine (XXVIII) with diazomethane gave 1, 2-dihydro-4-methoxycarbonyl-1-methyl-2-oxopyridine (XXIX), 6-methoxycarbonyl-3-methyl-2-oxo-3-azabicyclo [4. 1. 0] hept-4-ene (XXX), and 1, 2-dihydro-4-methoxycarbonyl-1, 3-dimethyl-2-oxopyridine (XXXI). The reaction of compound (XXIX) with diazoethane afforded 3-ethyl-1, 2-dihydro-4-methoxycarbonyl-1-methyl-2-oxopyridine (XXXII), 6α-methoxycarbonyl-3, 7β-dimethyl-2-oxo-3-azabicyclo [4, 1, 0]-hept-4-ene (XXXIII), and 1-ethyl-6-methoxycarbonyl-3, 7-dimethyl-2-oxo-3-azabicyclo [4. 1. 0] hept-4-ene (XXXIV). In case of the treatment of 5-carboxy-1, 2-dihydro-1-methyl-2-oxopyridine (XXXV) and 1, 5-dihydro-1, 5-dioxo-3H-oxazolo [3, 4-a] pyridine (XXXVIII) with diazomethane, 1, 2-dihydro-5-methoxycarbonyl-1-methyl-2-oxopyridine (XXXVI) and 1, 2-dihydro-6-methoxycarbonyl-1-methyl-2-oxopyridine (XXXIX) were obtained, respectively.
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荒田 義雄, 安田 信吾, 徳野 健次, 花岡 美代次
1976 年 24 巻 8 号 p.
1879-1883
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The Stevens rearrangement of the N-benzyl bromide (VII), derived from 1-oxoquinolizidine (V), afforded 9a-benzyl-1-oxoquinolizidine (VIII). Reduction of the methiodides (VI and IX) of V and VIII with sodium amalgam gave the ten-membered aminoketones (XII and XIII), respectively. The yield of XIII was much more excellent than that of XII, because of the influence of the C
9a-benzyl substituent in IX. The C
9a-benzyl substituent, however, produced little effect on the reductive cleavage in the Birch reduction of IX leading to XIII and XV in comparison with that of VI leading to XIV, though 9a-benzylquinolizidine methiodides (XIa and XIb) furnished the ten-membered amine (XVI) in considerable yields.
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上杉 晴一, 名倉 猛夫, 大塚 栄子, 池原 森男
1976 年 24 巻 8 号 p.
1884-1892
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Ultraviolet absorption and circular dichroism properties of ApUpG and its analogs in which the adenosine is modified are reported. The adenosine analogs include formycin (F), 8, 5'-S-cycloadenosine (
sA), 8, 2'-S-cycloadenosine (A
s), 8, 5'-O-cycloadenosine (
oA), 8, 2'-O-cycloadenosine (A
o), 8-bromoadenosine (Br-A) and 8-oxyadenosine (HO-A). S-and-O-Cyclonucleosides and F take torsion angles of anti type, while Br-A and HO-A assumed to take syn conformation in these analog trinucleotides. All analogs have very weak stacking interaction and show a tendency to form an aggregate at low temperature.
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小木曽 太郎, 久原 和憲, 野田 伸隆, 加藤 好夫
1976 年 24 巻 8 号 p.
1893-1901
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
An attempt has been made to clarify the action of drugs for liver disease, protoporphyrin (PP) and phosphorylcholine (PC) on the structure of liver microsomal membrane during carbon tetrachloride (CCl
4) intoxication, by measuring ultraviolet (UV) absorbance, infrared (IR) spectroscopy, circular dichroism (CD) and ribonucleic acid (RNA) content, and by using some hydrophobic probes, 1-anilinonaphthalene-8-sulfonate (ANS) and 2, 4, 6-trinitro-benzenesulfonate (TNBS). Administration of PC to CCl
4-poisoned rats was found to decrease the increased nonribosomal RNA content of the microsomes at 5 days, to some extent. ANS binding to microsomes little changed in all groups. A double reciplocal plot of ANS binding to the microsomes indicated that the affinity of the membrane of all groups for ANS was not affected by CCl
4 or the drug administrations. TNBS binding to the amino-phospholipids, phosphatidylserine (PS) and phosphatidylethanolamine (PE), however, on the membrane was extremely decreased in CCl
4-poisoned rats at 2 and 5 days, by 21-25% for PS and 25-34% for PE, as compared with those of control rats, indicating a significant alteration of the phospholipid composition in the membrane. Administration of PC for 8 days produced a significant increase in its binding to both aminophospholipids. It was found from CD spectra of the membrane that CCl
4 administered caused partially conformational changes of the proteins, significant at 5 days, and administration of PC to the poisoned rats for 5 days recovered the decreased ordered structure to the nativelevel. A semigraphical method of CD data analysis exhibited that the membrane contained approximately 55% α-helix, 21% β-structure and 24% unordered structure and CCl
4 administration decreased the helix content by 9% without significant alteration of β-structure. IR spectra also indicated that the membrane contained β-structure. PP had no appreciable effects on the structure of the membrane. Thus, it is concluded that PC has an excellent reconstructive action of phospholipid and protein structure of the injured microsomal membrane.
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山川 浩司, 金親 肇
1976 年 24 巻 8 号 p.
1902-1908
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Unsymmetrical β-diketonate metal (III) chelates, tris (formylacetonato) cobalt (III) and-chromium (III) chelates, were synthesized. Fac and mer isomers of these chelates were separated by column chromatography, and the stereochemistry of paramagnetic cobalt (III) chelate is discussed from nuclear magnetic resonance (NMR) spectra. Electrophilic substitution reactions (chlorination, bromination, iodination, nitration, and thiocyanation) of the fac and mer isomers of these chelates were successful. Infrared, ultraviolet, and NMR spectra were measured for these chelates.
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山原 條二, 木島 孝夫, 榊原 弥生, 石黒 真紀子, 沢田 徳之助, 藤村 一
1976 年 24 巻 8 号 p.
1909-1912
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Tetrahydropalmatine is known to have potent sedative and hypnotic action and the depressant effect on the central nervous system of some compounds to realted berberine was tested. The levorotatory isomer of tetrahydroberberine had a stronger activity among the synthesized compounds.
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奥本 武城, 今村 博
1976 年 24 巻 8 号 p.
1913-1916
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Improsulfan had the topical antitumor activity against Yoshida sarcoma cells, in comparison with cyclophosphamide. The mean survival time of rats bearing the tumor treated intraperitoneally with each optimal dose of improsulfan (10 mg/kg/day) or cyclophosphamide (5 mg/kg/day) from day 3 for 2 weeks was 32.2 or 31.7 days, respectively. In the sequential treatment of the two drugs, the mean survival time of the group administered with improsulfan for the first week and with cyclophosphamide for the second week was 46.3 days, which was the longest day among all of the groups tested. The therapeutic effect may be improved even by combinations of alkylating agents.
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千賀 慶太郎, 金森 由香子, 西垣 貞男, 米田 文郎
1976 年 24 巻 8 号 p.
1917-1921
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
A new synthetic method of 2-vinyl-v-triazolo [4, 5-d] pyrimidines, which consists of the nitrosative cyclization of 1, 3-dimethyl-6-(α-methylalkylidenehydrazino) uracils with a mixture of N-nitrosodimethylamine and phosphorus oxychloride (NDA+POCl
3) is described. The reaction of 1, 3-dimethyl-6-hydrazino-5-nitrosouracil with acetophenone gave 1, 3-dimethyl-6-phenyl-7-azalumazine (3-phenylfervenulin) (X). The nitrosation of 6-benzylidenehydrazino-1, 3-dimethyluracil with NDA+POCl
3 also gave X.
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原 博, 星野 修, 梅澤 文輔
1976 年 24 巻 8 号 p.
1921-1925
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
By the treatment of the p-quinol acetate (Xa) and (Xb) with trifluoroacetic acid, (±)-10-benzyloxy-1-hydroxy-2, 9-dimethoxyaporphine (XIa) and (±)-9-benzyloxy-1-hydroxy-2, 10-dimethoxyaporphine (XIb) were given in good yield, respectively. Furthermore, XIa and XIb were converted to (±)-bracteoline (XIIa) and (±)-isoboldine (XIIb) by catalytic debenzylation, or to (±)-10-hydroxy-1, 2, 9-trimethoxyaporphine (XIVa) and (±)-N-methyllaurotetanine (XIVb) by methylation and successive debenzylation, respectively.
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岡田 芳男, 谷 昇平, 八渡 裕子, 柳生 正見
1976 年 24 巻 8 号 p.
1925-1927
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
As analogues of D-cycloserine, the part structure of penicillin and D-D carboxypeptidase substrate of peptidoglycan of bacterial cell wall, D-alanine derivatives and their stereoisomers and D-alanyl-D-alanine derivatives and their stereoisomers (R
1-Ala-R
2, R
1-Ala-Ala-R
2 : R
1=Z, H ; R
2=NHNH
2, NHCH
3, NHCH
2CH
2OH) were synthesized. All compounds obtained did not show any antibacterial activity against Staphylococcus aureus, Sarcina lutea, Pseudomonas aeruginosa and Escherichia coli.
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竹下 徹, 石本 祐男, 池川 信夫
1976 年 24 巻 8 号 p.
1928-1931
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Desmosteryl acetate, a useful key intermediate for synthesis of the metabolites of vitamin D
3, was synthesized from fucosterol by two routes ; (1) 24, 28-epoxyfucosteryl acetate was treated with solid acids such as zeolite, silica-alumina and alumina-boria to give desmosteryl acetate in a yield of 16%-40%, (2) dehydration of 24-hydroxycholesteryl acetate, which was obtained by ozonolysis of fucosteryl acetate followed by reduction with sodium borohydride, with P
2O
5 in benzene afforded desmosteryl acetate in a yield of 85%.
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山川 浩司, 金親 肇
1976 年 24 巻 8 号 p.
1931-1934
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Introduction of chlorine, bromine, and iodine atom into the ring of labile bivalent metal acetylacetonates, bis (acetylacetonato) nickel (II) and-cobalt (II) chelates, is effected by N-halosuccinimide in carbon tetrachloride. Infrared and ultraviolet spectra of halogenated metal (II)-acetylacetonate chelate derivatives were measured. The masses of substituent at the central carbon atom of these metal (II)-acetylacetonates affected the frequencies of C=O and C=C stretching bands.
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金親 肇, 山川 浩司
1976 年 24 巻 8 号 p.
1934-1935
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The reaction of bis (o-phenylenediamine) nickel (II) chloride and acetylacetone is examined and bis (acetylacetonato) (o-phenylenediamine) nickel (II) chloride dihydrate and 2, 4-dimethyl-1, 5-benzodiazepinium chloride were isolated.
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森本 俊明, 関屋 実
1976 年 24 巻 8 号 p.
1935-1938
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
It has now been found that trichloroacetyl chloride is capable to react with Schiff bases in the presence of triphenylphosphine to give 3, 3-dichloro-2-azetidinones. Mechanistically the reaction appears to involve the chlorine cation extraction from the initially formed adduct by triphenylphosphine.
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菊川 靖雄, 横山 祐作
1976 年 24 巻 8 号 p.
1939-1943
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Sodium acetanilidoborohydride prepared from acetanilide and sodium borohydride in α-picoline reduced acid chlorides to alcohols in dichloromethane. On the other hand, this reducing reagent prepared in pyridine did not reduce acid chlorides but reduced the pyridine ring to give acylpiperidines.
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内藤 俊一, 塩田 喜代子, 沢田 まち子, 二木 賞子, 粟田口 幹男, 水谷 光雄
1976 年 24 巻 8 号 p.
1943-1947
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
The laxative action of bis (p-hydroxyphenyl) pyridyl-2-methane disulfate is considered to be dependent on the formation of the free phenolic compound, bis (p-hydroxyphenyl)-pyridyl-2-methane by hydrolysis. Therefore, the activity of the parent compound as a laxative must be governed by arylsulfatase activity in the human intestine. When examinations of human feces were made, arylsulfatase activity in the intestine was detected, and about 98% of the samples were shown to be positive. Validity of the fecal arylsulfatase test in the test population might be supported by the liquefaction test of rat feces with the injection of the parent compound into duodenum.
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森崎 益雄, 坂内 清, 池川 信夫
1976 年 24 巻 8 号 p.
1948-1949
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Oxymercuration-demercuration of 3β-acetoxycholesta-1, 5-diene (2) followed by saponification gave 2β-hydroxycholesterol (3) and 1α-hydroxycholesterol (4) in 14% and 26% yield, respectively.
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佐藤 大助, 橋本 敏弘
1976 年 24 巻 8 号 p.
1950-1953
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Reduction of 16-anhydrogitoxigenin 3-acetate (II) with NaBH
4-transition metal chloride systems as well as with transition metal hydrides gave geometrically isomeric card-17 (20)-enolides, V and VI, new type of cardenolide. Stereochemistry of the products was discussed on the basis of Cotton effect,
1H-and
13C-nuclear magnetic resonance spectra. The structure and ratio of the products varied depending on the kind of transition elements.
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谷川 啓一
1976 年 24 巻 8 号 p.
1954-1956
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
A difference in detection sensitivity of β-diketone metal chelates by gas chromatography is produced by the difference in the metal present, irrespective of the difference in ligands or of detectors and the reason for it was examined by gas chromatography-mass spectrometry (GC-MS). When the chelates of copper (II) and iron (III), which show poor sensitivity in gas chromatography, were introduced directly into the ion source of a mass spectrometer, their ionic intensity was large but the ratio of molecular ion to total ion was smaller than that of the chelates of rhodium (III) and chromium (III), which show good detection sensitivity. When the sample was heated for gasification and collected in a gas reservoir for mass spectrometry, chelates of copper (II) and iron (III) showed great disintegration of the molecular ion and a large number of fragment ion species was produced. Ratio of molecular ions to total ions was greater in rhodium (III) and chromium-(III) chelates, with smaller number of fragment ions. Thus the difference in detection sensitivity according to the kind of a metal present was related to the ratio of molecular ions present to total ions of the metal chelates, and the difference in the detection sensitivity of β-diketone metal chelates in gas chromatography is affected largely by thermal stability of the chelates rather than by ionization efficiency of flame ionization detector and electron caputure ionization detector or to the stability of these chelates to ionization.
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吉井 英一, 小泉 徹, 川添 敏司
1976 年 24 巻 8 号 p.
1957-1958
発行日: 1976/08/25
公開日: 2008/03/31
ジャーナル
フリー
Ketene triethylsilyl methyl acetals obtained by hydrosilation of α, β-unsaturated esters were reacted with phenyl (bromdichloromethyl) mercury to give homologated 2-chloroacrylates
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