巻号一覧
90 巻, 7 号
選択された号の論文の21件中1～21を表示しています
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白木 弥寿之, 菅野 茂, 池田 喜明1970 年 90 巻 7 号 p. 785-795
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーPharmacological examinations were made on the action of 7-{2-hydroxy-3-[4-(p-chlorobenzyl) piperazino] propyl} theophylline (SP-1131) on the circulation system, using aminophylline as the control agent, with dogs and rats. Intra-arterial and intravenous administration of SP-1131 in coronary and femoral arterial perfusion in a dog elicited strong increase in coronary blood flow and transitory increase in femoral arterial blood flow. Increased flow of coronary arterial blood was markedly observed in heart-lung preparation test. Intravenous administration of SP-1131 resulted in slight variation of blood pressure and increased heart rate in normal and spinal dogs but the action was weaker than that of theophylline. In the constant pressure perfusion experiments with mesenteric artery and renal artery of the dog, SP-1131 increased blood flow when given intra-arterially but decreased renal blood flow when given as an intravenous injection. Experiments with the rat did not show oliguria action. In the heart-lung preparation experiments with the dog, SP-1131 decreased the cardiac minute volume and heart beat, showing that it had no action of myocardial stimulation. Consequently, the mechanism of the action of SP-1131 on blood pressure and increasing heart beat seems to differ in some respects from that of theophylline. It was considered that its action on dilating coronary blood vessels might not be due to the secondary factor accompanying accelerated myocardial metabolism.抄録全体を表示PDF形式でダウンロード (1247K) -
小倉 治夫, 杉本 信吾, 志村 喜孝1970 年 90 巻 7 号 p. 796-799
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーThirty N-substituted 2-aminobenzothiazoles and 2-aminobenzoxazoles have been synthesized for the purpose of mass measurement. The structure of all the compounds was determined by infrared and mass spectra.抄録全体を表示PDF形式でダウンロード (451K) -
中西 美智夫, 岡田 忠夫, 津曲 立身1970 年 90 巻 7 号 p. 800-807
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーA new derivative of phenothiazine, 8-[3-(2-chloro-10-phenothiazinyl) propyl]-1-thia-4, 8-diazaspiro [4, 5] decane-3-one hydrochloride (APY-606), was examined for its pharmacological activities in comparison with chloropromazine and thioridazine as the standard compounds. APY-606 has a potent sympatholytic action with a low toxicity, although it is a phenothiazine derivative. APY-606 has a characteristic spectrum of pharmacological activities, which differs from those of standard compounds. This compound may prove to be a new type agent having a psychotropic activity in clinical use.抄録全体を表示PDF形式でダウンロード (809K) -
中西 美智夫, 岡田 忠夫, 加藤 安之1970 年 90 巻 7 号 p. 808-812
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーA spectrophotometric method (UV-method) for quantitative determination of a new phenothiazine derivative, 8-[3-(2-chloro-10-phenothiazinyl) propyl]-3-oxo-1-thia-4, 8-diazaspiro [4, 5] decane hydrochloride (APY-606) in rat urine was investigated. By ultraviolet (UV)-method less than 1.5% of the given dose was found in the urine during the 3 days following the administration of this compound in rats. Most of the urinary excreta measured by UV-method, however, seemed to derive from the metabolites of APY-606, since unchanged APY-606 was not detected in rat urine by thin-layer chromatographic analysis. Four metabolites of APY-606 were detected in rat urine by thin-layer chromatography. One of them was found to be phenothiazine s-oxide of APY-606, and another one was supposed to have a hydroxy group from its color reaction. Three metabolites were also detected, but the native compound was not found in the bile.抄録全体を表示PDF形式でダウンロード (532K) -
今村 博, 岡田 忠夫, 松井 英一, 加藤 安之1970 年 90 巻 7 号 p. 813-817
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーTritium labeled compound (3H-APY-606) of a new phenothiazine derivative, 8-[3-(2-chloro-10-phenothiazynyl) propyl]-3-oxo-1-thia-4, 8-diazaspyro [4, 5] decane hydrochloride was synthetized, and its absorption, distribution, excretion and metabolism were investigated in rats. When this compound was orally administered at a dose of 10 mg/kg, about 40% of the dose was absorbed from the gastrointestinal tract within 6 hr, but the speed of absorption was relatively slow. 3% and 55% of the administered radioactivity (3H) were excreted in the urine and feces, respectively, during the 3 days following the oral administration of 3H-APY-606, and 32% of the dose was also excreted in the bile during 24hr. The highest concentration of 3H in most organs was found 4 hr after its oral administration, and 3H was concentrated in the liver, adrenals, kidney and lung. 3H level in the brain was 2-4 fold of that in the blood, and blood level was relativery low. Protein binding of 3H in the serum was 90% at 1 hr, 34% at 24 hr, after oral administration. Seventy % of 3H in the urine and 94% of it in the bile were extracted with organic solvent, and a small amount of glucuronide was formed in the urine. Four radioactive metabolites in the urine and 3 metabolites in the bile were detected by thin-layer chromatography, but the native compound could not be detected.抄録全体を表示PDF形式でダウンロード (611K) -
西村 温樹, 永井 保嵩, 鈴木 隆, 沢山 忠弘1970 年 90 巻 7 号 p. 818-828
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリー3, 3-Disubstituted-1, 2, 3, 4-tetrahydroquinoline-2, 4-diones were prepared by alkylation of 3-substituted-4-hydroxy-2 (1H)-quinolones or cyclization of 2, 2-distubstituted malonanilic acids with PPA. Degradation of 3-nitro-3-phenyl-1, 2, 3, 4-tetrahydroquinoline-2, 4-dione(XXV) was studied as shown in Chart 2. Synthesis of 3-phenyl-4-hydroxy-2 (1H)-quinolone (XI) derivatives having substituted benzene, and aminoalkylation and acylation of XI were carried out. The deshielding influence of 4-hydroxy group of 4-hydroxy-2 (1H)-quinolones to 5-proton in nuclear magnetic resonance (NMR) spectra was discussed.抄録全体を表示PDF形式でダウンロード (1004K) -
亀山 勉, 丹羽 弘司, 木皿 憲佐, 岩泉 弘子1970 年 90 巻 7 号 p. 829-834
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーExaminations were made on the absorption through the digestive tract and systemic distribution of 1, 3-diphenyl-5-(2-dimethylaminopropionamido) pyrazole hydrochloride (AP-14·HCl) using rats and the following results were obtained. AP-14·HCl is well absorbed through the digestive tract and 90% of the amount administered is absorbed within 2 hr after its oral administration. This absorption is mainly made through the small intestine and it was thought that this easy absorptivity is due to the high oil/water distribution ratio in the intestinal wall and because this chemical dissolves inside the small intestinal wall. Blood level of AP-14 is low, probably because it has little ability to bind with serum proteins. AP-14 also transits rapidly to fat tissues. Duration of the analgesic effect of AP-14 was found to parallel the concentration of AP-14 in the brain.抄録全体を表示PDF形式でダウンロード (599K) -
栗原 藤三郎, 武田 秀雄, 伊藤 秀雄, 鈴木 稠徳1970 年 90 巻 7 号 p. 835-840
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーSince sodium colistinmethansulfonate (1) gives the positive colour reaction of the primary amines, the existence of free amino radical in its molecule is suggested. In order to investigate the differences of five amino radicals in colistin, (1) was dinitrophenylated with dinitrofluorobenzene (DNFB) and the dinitrophenylated-1 was hydrolyzed with HCl to afford six partial peptides. The arrangements of amino acids were decided by the determination of the composition of amino acids, C-terminal amino acids and N-terminal amino acids in each peptide. The γ-amino radical of diaminobutyric acid next to L-leucine was proved to be dinitrophenylated. On the other hand, colistin sulfate and colistin base were mono-dinitrophenylated with one molar DNFB and the consequent DNP-colistin was partially hydrolyzed. The arrangements of the amino acids of these partial peptides were decided by the same method as in (1). 6-methyl-octanoic acid was found by gas chromatography in all these peptides. From these data, it is assumed that the γ-amino radical of the terminal diaminobutyric acid in the side chain tripeptide would be the most reactive radical and the γ-amino radical of the diaminobutyric acid adjoining L-leucine would be the most inactive amino radical in the colistin molecule.抄録全体を表示PDF形式でダウンロード (619K) -
久保田 晴寿, 興津 孝雄, 鯉田 義之1970 年 90 巻 7 号 p. 841-845
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリー2-Alkylthio-5-(2-pyridyl)-1, 3, 4-thiadiazoles (R : CH3-C4H9) and 2-alkylthio-5-(3-pyridyl)-1, 2, 4-thiadiazoles (R : CH3, C2H5) were synthesized by cyclization of the corresponding alkyl 3-aroyldithiocarbazates with concentrated sulfuric acid. Oxidation of 2-alkylthio-5-pyridyl-1, 3, 4-thiadiazoles with potassium permanganate gave the corresponding 2-alkylsulfonyl-5-pyridyl-1, 3, 4-thiadiazoles. It was found that the cyclization product of potassium 3-picolinoyl dithiocarbazate with concentrated sulfuric acid is mainly 2-pyridyl-1, 3, 4-thiadiazolin-5-thione rather than the thiol compound, by comparing the ultraviolet absorption spectra of the compound with those of N-and S-methyl derivatives which were obtained by methylation of the product with diazomethane.抄録全体を表示PDF形式でダウンロード (630K) -
村上 孝夫, 陳 秋明1970 年 90 巻 7 号 p. 846-849
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーFrom the ether extract of the whole herb of Centipeda minima O. KUNTZE (Compositae), taraxasteryl palmitate (I), taraxasteryl acetate (II), taraxasterol (III), stigmasterol (IV) (contaminated with β-sitosterol), and arnidiol (V) were isolated and identified. An unknown pentacyclic triterpenoid diol (VI), mp 204 -206°, C30H50O2, was also isolated and its structure was discussed from spectroscopic evidences.抄録全体を表示PDF形式でダウンロード (492K) -
井手 明雄, 重実 桂助, 重実 鈴, 溝口 富茂, 斎藤 清一1970 年 90 巻 7 号 p. 850-858
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーIn order to find competitive inhibitors of renin, 35 peptides having phenylalanyl-histidyl or leucyl-leucyl bond at the C-terminal, in the middle position or at the N-terminal of the peptide chain, were synthesized and leucylleucylvalyltyrosine methyl ester and leucylleucylvalylphenylalanine methyl ester were found to be active.抄録全体を表示PDF形式でダウンロード (1047K) -
白井 秀明, 早崎 孝則1970 年 90 巻 7 号 p. 859-862
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーReaction of imidazo [4, 5, 1-kl] phenoxazine (I) with trimethylsulfoxonium iodide (TMSI), prepared from DMSO with methyl iodide, in DMSO at 105° under nitrogen atmosphere gave 2-methyl-1, 2-dihydroimidazo [4, 5, 1-kl] phenoxazin-1-one (III). Similar reaction of I with TMSI in propanol or diethylene glycol afforded 1-methyl-(formyl) aminophenoxazine (V). The synthetic mechanisms of III and V were clarified.抄録全体を表示PDF形式でダウンロード (450K) -
福島 清吾, 黒柳 正典, 上野 明, 赤堀 幸男, 斎木 保久1970 年 90 巻 7 号 p. 863-869
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーCurzerenone, C15H18O2, [α]D ±0°, a main component in the essential oil of Curcuma Zedoaria, was found to have a planar structure Ia, on the basis of its mass, ultraviolet (UV), and nuclear magnetic resonance (NMR) spectra, along with spectral data of dihydro- and tetrahydro-curzerenone, and the perbenzoic acid oxidation product of I. Catalytic hydrogenation of I with platinum black in acetic acid gave two epimeric isomers (XII and XIII) of eleman-6-one. These facts show that the stereostructure of curzerenone can be written as I.抄録全体を表示PDF形式でダウンロード (698K) -
加藤 鉄三, 山中 宏, 平沼 英敏1970 年 90 巻 7 号 p. 870-876
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーThe Vilsmeier reaction (POCl3 and dimethylformamide) on the active methyl group in pyrimidine derivatives was examined with 4-methyl-2-phenyl-(IIIa), 4-methyl-6-phenyl-(IIIb), 2-methyl-4-phenyl-(IIIc), and 4-methyl-pyrimidine (IIId). These compounds all afforded the corresponding malonaldehyde compounds (Va-d) in a fair yield. In the case of IIId, a minute amount of 4-aminopyridine-3-aldehyde (VIII), formed by the recyclization of the ring, was obtained. Similar reaction was carried out with 2, 6-dimethyl-4-pyrimidone (IIIf), and 4-chloro-2, 6-dimethyl-(IIIg), and 2, 6-dimethyl-4-dimethylamino-pyrimidine (IIIh). IIIf and IIIg afforded 4-dimethylamino-2-methylpyrimidine-6-malonaldehyde (XI) produced by the attack on the methyl group in 6-position, and IIIh afforded the isomer (XII) of XI formed by the attack on the methyl group in 2-position.抄録全体を表示PDF形式でダウンロード (740K) -
加藤 鉄三, 山中 宏, 平沼 英敏1970 年 90 巻 7 号 p. 877-882
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーNitrosation in liquid ammonia was examined with eight kinds of pyrimidine derivatives with a methyl group in 4-position, such as 4, 6-dimethyl-(Ia), 2-ethyl-4-methyl-(Ib), 2, 6-diethoxy-4-methyl-(Ic), and 6-methoxy-4-methyl-2-phenyl-pyrimidine (Id), and the methyl in 4-position was found to transit to aldoxime or acid amide in a good yield. In the case of 2-benzyl-4-methoxy-6-methylpyrimidine (Ij) and 4-methoxy-5, 6, 7, 8-tetrahydroquinazoline (VII), nitrosation occurred in the active methylene and the corresponding ketoximes were obtained.抄録全体を表示PDF形式でダウンロード (582K) -
伊東 宏1970 年 90 巻 7 号 p. 883-892
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーThe essential oils in the leaves of 110 samples of genus Perilla were analyzed by gaschromatography and they were classified into four chemical groups, containing (1) mainly perillaldehyde and its related compounds, (2) furyl ketone derivatives, (3) phenylpropanoids, and (4) citral. These results were applied to the evaluation of perilla leaves.抄録全体を表示PDF形式でダウンロード (752K) -
安江 政一, 加藤 武, 榊原 仁作1970 年 90 巻 7 号 p. 893-898
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーLyoniol-A (I), the main component of the toxic principles of Lyonia ovalifolia var. elliptica, was identified as lyoniatoxin.5) The structure of lyoniol-A (lyoniatoxin) was concluded as (I) through the reactions shown in Fig. 3 and from the physical data of the reaction products. Alkaline hydrolysis of I gave deacetyllyoniol-A, a pentahydric alcohol, which was proved to be identical with lyoniol-B (II), a minor constituent. II formed monoacetonide (IV) which did not react with chromic acid. Thus, the remaining three hydroxyl groups must be tertiary. II consumed one mole of sodium periodate but I did not. Chromic acid oxidation of I gave a monoketone (III), which was believed to be a six or more membered cyclic ketone from its IR spectrum. These results and nuclear magnetic resonance (NMR) data of I, II, and III suggested that I has a partial structure of 〓C-CH (OAc)-CH (OH)-C〓. Lithium aluminum hydride reduction of I or II gave dihydrolyoniol-B (V), which was derived to its triacetate (VI) with acetic anhydride and pyridine. These reactions suggested that I has an epoxide ring in its molecule and the epoxide group was reduced to an alcoholic group. When V was treated with p-toluenesulfonic acid in acetone, dihydrolyoniol-B acetonide (VII), dihydrolyoniol-B anhydroacetonide-I (VIII), and dihydrolyoniol-B anhydroacetonide-II (IX) were produced. VII afforded monoacetate on mild acetylation. Chromic acid oxidation of IX gave a cyclopentanone derivative X. Thus, the epoxide ring must be situated in the cyclopentane ring. Because of a close relationship between the plant source and similarity in biological activity, lyoniol-A seems to have the same carbon skeleton and a very similar stereostructure as grayanotoxin-I8) and rhodojaponin-II.9) Thus, the structure of lyoniol-A should be represented by formula I. From the coupling constant of C6-H and C7-H, and specu lation about stereo models, it was concluded that C6-H and C7-H are trans and, therefore, the C7-hydroxyl group must be in α-configuration. The structures of IX and VIII were assumed to be △10, 20-ene-6, 7-acetonide (20-terminal methylene protones) and △15, 16-ene-6, 7-acetonide (allyl coupling of 17-methyl), respectively.抄録全体を表示PDF形式でダウンロード (708K) -
高木 信也, 許 鴻源, 竹本 常松1970 年 90 巻 7 号 p. 899-902
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーAmino acid composition of Formosan seaweed, Petalonia fascia (Muller) KUNTZE (Scytosiphonaceae), was examined. As the characteristic amino acids, a neutral amino acid, named petalonine, mp 182-184° (decomp.), C4H9O3N, was isolated besides laminine and pipecolic acid. Chemical structure of petalonine was found to be N-(2-hydroxyethyl) glycine from its elemental analysis and synthesis.抄録全体を表示PDF形式でダウンロード (505K) -
谷 千秋, 今西 勇, 西庄 重次郎1970 年 90 巻 7 号 p. 903-905
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーIn continuation of the preceding work, 1) the quaternary base fraction was reduced with sodium borohydride and the product thereby obtained was found to be dl-capaurimine. Since this substance is a reduction product, it was considered to be present in the plant in the form of dehydrocapaurimine. This is the first time that the presence of such a form was presumed.抄録全体を表示PDF形式でダウンロード (428K) -
三宅 良一, 矢島 尚1970 年 90 巻 7 号 p. 905-907
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーA thiocyanogen solution can be stabilized for a few months when it is made free from ferric ion, which is introduced as impurity from commercial salts of thiocyanate. At the same time, lead thiocyanate, the intermediate in the preparation of a thiocyanogen solution, also becomes stable to photodecomposition by the removal of ferric ion. Elimination of ferric ion was guaranteed by steam distillation of hydrogen thiocyanate at a reduced pressure and the distillate was introduced into a lead acetate solution.抄録全体を表示PDF形式でダウンロード (429K) -
森 逸男1970 年 90 巻 7 号 p. 908-912
発行日: 1970/07/25
公開日: 2008/05/30
ジャーナル フリーExaminations were made on the absorption spectrophotometric determination of I- and NO2- using 3, 4, 5, 6-tetrachloro-3', 4', 5', 6'-tetrahydroxyfluoran methyl ester (Cl-gall-CH3). For the determination of I-, calibration curve of 0.1 -0.6 μg/10 ml of I- was prepared with 1.0 ml of 1.0×10-2 cetylpyridinium chloride, 1.0 ml of 20% H2O2 solution, and 1.0 ml of 1.0×10-3M Cl-gall-CH3 solution, in sulfuric acidity, brought to 10 ml with water and the same solution added with definite amount of I- by measuring their optical density at 510 mμ. For the determination of NO2-, the calibration curve was prepared with 0-18.4 μg/10 ml of NO2- with 1.0 ml of 1.0% poly vinyl alcohol and 1.0 ml of 1.0×10-3M Cl-gall-CH3 solution brought to 10 ml with water and heated at 60° for 10 min and the same solution added with definite amount of NO2- by measuring their optical density at 490 mμ. Determination of NO2- was little interfered by other ions but any ion present gave negative error in the determination of I-.抄録全体を表示PDF形式でダウンロード (506K)
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