巻号一覧
98 巻, 5 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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岩鶴 素治, 関口 慶二1978 年 98 巻 5 号 p. 557-562
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe protein binding of Naphthol Yellow S to bovine serum albumin (BSA) was examined and three pairs of parameters (binding numbers and constants) were obtained by equilibrium dialysis and Scatchard plot. These were n=1, 2, and 8, and ∞ (experimentally), 2.4×105M-1, and 1×103M-1, respectively. Though the spectra of Naphthol Yellow S showed change in absorbance by addition of BSA and the spectra with or without BSA intersected each other at a certain wavelength, not showing an isosbestic point. The results from equilibrium dialysis showed that two classes of binding were contributing greatly to the spectral change. An attempt was made to estimate the molar absorptivities of these two species. The calculated absorbances from the molar absorptivities of free or bound dye and their concentrations agreed well with those of observed. Thus the inference validity was ascertained. When the protein bindings are studied spectrophotometrically, the molar absorptivities should also be taken into consideration as so many classes if they have two or more binding classes. In the system of Naphthol Yellow S-BSA, the third binding was weak and masked by the first and second bindings, and the molar absorptivity of the third binding was not obtained as yet.抄録全体を表示PDF形式でダウンロード (649K) -
諏訪 要1978 年 98 巻 5 号 p. 563-568
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーDiametral impact compression test and impact bending test were carried out using a hammer type impact tester to estimate impact strength of tablets. The hardness, which represents a static compression strength of a tablet, was also determined by the Schleuniger hardness tester. All the tablets used were formulated in the laboratory and, based on weight, thickness, and apparent density, they were classified into five groups. The impact force for breaking 50% of tablets (F50) and the impact tensile strength (σI) were used as indices of the impact strength and these values were compared with hardness of the tablet. The data obtained supported following conclusions. 1) It is possible to estimate the impact strength by determining F50, which showed the same tendency as hardness of the tablet. 2) Both the impact and static tensile strengths were proportional to hardness, when the thickness of a tablet was almost the same. 3) Proportional relationship was also suggested between the static and impact tensile strength of the tablet, having almost the same thickness. However, in the case of tablets having similar apparent density and different thickness, the relationship was not observed and the impact tensile strength was almost constant.抄録全体を表示PDF形式でダウンロード (668K) -
志野木 正樹, 森 五彦1978 年 98 巻 5 号 p. 569-576
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーCultivated cannabis was divided into eight parts. The nondestructive neutron activation analysis using the monostandard method was applied to the each of leaves, male flower, and seed. Thirty-five kinds of elements were determined by this method from each sample. Following items on 29 kinds of elements, which were determined in most part of cannabis, were discussed : (1) Comparison of male and female cannabis, (2) comparison of the coefficient of variation among each part of cannabis, and (3) discussion on the elemental distribution pattern. On the basis of element concentration, the distribution pattern was divided into the following four classes : (1) Upper part<middle part<lower part. Al, Ba, Br, Ca, Cl, Cr, Fe, I, Sc, and rare earth elements belong to this pattern. (2) Upper part<middle part<lower part. Co, Cs, and Rb belong to this pattern. (3) Upper part=middle part=lower part. K, Mg, Mn, Na, and Zn belong to this pattern. (4) Others. Hg, In, and Sb belong to this pattern.抄録全体を表示PDF形式でダウンロード (705K) -
中垣 正幸, 市橋 等1978 年 98 巻 5 号 p. 577-584
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe egg lecithin (PC) monolayer was spread on an aqueous butanol or hexanol solution, and the surface pressure-molecular area curves were obtained. From the increase of surface pressure by penetration of alcohol molecules into lecithin monolayer, the amount, penetrated or adsorbed amount, was calculated from the following equation [numerical formula] and the adsorption isotherms of Langmuir type were obtained. The amount of saturated adsorption of alcohol and k, the parameter which represents the affinity of adsorption, were calculated from the linear relation between C/T and C (alcohol concentration). The saturated amount of alcohol decreased with increase in surface concentration of lecithin, but k became minimum. This was explained by the cavity model. The lecithin monolayer penetrated by alcohol molecules forms a mixed monolayer of lecithin and alcohol. The mean area of mixed monolayer was larger than the area calculated by assuming additivity of the area of each component. It was concluded that alcohol molecules penetrating into the lecithin monolayer decrease the cohesive force between lecithin molecules.抄録全体を表示PDF形式でダウンロード (836K) -
浜田 喜樹, 伊藤 義雄1978 年 98 巻 5 号 p. 585-592
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーN-Alkylation of 10H-pyrido [3, 2-b]-[1, 4]-benzoxazine (I) was examined both in alkaline and neutral media. 10-Alkyl-10H-pyrido [3, 2-b]-[1, 4]-benzoxazine derivatives were easily obtained by the reaction of I with a variety of alkyl halides (methyl iodide, isobutyl bromide, dimethylaminopropyl chloride, etc.) in dimethylformamide, in the presence of sodium hydride. 10-Methyl-10H-pyrido [3, 2-b]-[1, 4]-benzoxazine (XI) was prepared by this method. Reaction of I with methyl iodide in acetone afforded the corresponding quaternary salt. 1-Methyl-1H-pyrido [3, 2-b]-[1, 4]-benzoxazine (XXIII) was obtained by the treatment of this quaternary salt with sodium carbonate solution. The compounds XI and XXIII were used as models for the amino and imino tautomers of I, and ultraviolet spectra of these model compounds were compared. The spectral data show that the amino tautomer is preferred in both cyclohexane and methanol. The selective alkylation pathways of I were discussed with some evidence and speculations.抄録全体を表示PDF形式でダウンロード (826K) -
木原 勝, 小林 茂, 新宮 徹朗1978 年 98 巻 5 号 p. 593-599
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーStudies on nuclear magnetic double resonance (NMDR) and homonuclear INDOR spectra of the apogalanthamine analogs indicated that the azocine ring in the apogalanthamine analogs existed predominantly in a half-tub conformation.抄録全体を表示PDF形式でダウンロード (801K) -
川田 俊展, 原野 一誠, 田口 胤三1978 年 98 巻 5 号 p. 600-604
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーAn experiment was carried out to confirm the reaction mechanism involving the formation of a carbonium ion which had been postulated previously for the catalytic rearrangement of O, S-dialkyl dithiocarbonates to S, S-dialkyl dithiocarbonates with Lewis acid. Optically active S-methyl O-2-octyl dithiocarbonate underwent rearrangement catalytically to S-methyl S-2-octyl dithiocarbonate with racemization. Kinetic study of the catalytic rearrangement of O-butyl S-methyl dithiocarbonate showed that the reaction rate was proportional to the concentrations of both O, S-dialkyl dithiocarbonate and the catalyst. The rate constants of O-alkyl S-methyl dithiocarbonates (ROCSSCH3) increased in the order of alkyl groups (R) of iso-Pr>Me≈Et≈n-Pr≈n-Bu. These chemical and kinetic observations support the postulated carbonium ion mechanism.抄録全体を表示PDF形式でダウンロード (599K) -
田中 千秋, 西田 元信1978 年 98 巻 5 号 p. 605-610
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーBenzyl 2-oxazolecarbamates (I), 2-aminoxazoles (II), 1-benzyloxycarbonyl-3-alkylureas (III), alkylureas (IV), (E)-alkenylureas (V), and 2-amino-2-oxazolines (VI) were treated with trifluoroacetic anhydride, and determined by programmed temperature gas chromatography. Acetyl derivatives (VIIa-Xa) of IIa, IVa, Va, and VIa were converted into trifluoroacetyl derivatives by treatment with trifluoroacetic anhydride. To examine the route of hydrogenation of I, 5-phenyl (Ia), 5-methyl (Ib), 5-isopropyl (Ic), 5-tert-butyl (Id), 4-methyl-5-phenyl (Ie), and 4-isopropyl-5-phenyl derivative (If) of I were submitted to catalytic reduction over palladium-carbon or platinum oxide, and then these products were determined at appropriate intervals. The bulkiness of substituents was found to give some marked effect on ring fission.抄録全体を表示PDF形式でダウンロード (658K) -
田中 千秋1978 年 98 巻 5 号 p. 611-617
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーIn confirmation of reduction intermediates, various 2-aminoxazoles (I) and 2-acetamidoxazoles (XIV) were submitted to catalytic reduction. In the hydrogenolysis of I, ring cleavage occurred in competition with the addition of hydrogen to the C (4)-C (5) double bond. When using palladium-carbon or platinum oxide catalyst, 4-phenyl-5-alkyl-I was mainly converted to alkylureas (IV) via (E)-alkenylureas (II), and 5-phenyl-I was converted to IV via II and 2-amino-2-oxazolines (III). When using platinum oxide catalyst, 4- or 5-alkyl-I was largely converted to IV via II. In both 4-phenyl-5-alkyl-I and alkyl-I, III was obtained as a by-product. The mechanism of the hydrogenolysis of I was also examined.抄録全体を表示PDF形式でダウンロード (776K) -
高橋 浩, 野口 博美, 富田 考一, 乙益 寛隆1978 年 98 巻 5 号 p. 618-622
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe chiral hydrazone compounds (IVa and IVb) were obtained by the condensation of methyl pyruvate and ethyl phenylglyoxylate with l-ephedrine-N-amine. Reduction of the C=N group in these compounds was carried out using Pd-C (10%) catalyst in ethanol at room temperature, followed by hydrogenolysis of the N-N linkage using the same catalyst in acidic ethanol solution under pressure of 3-4 kg/cm2 at 50-60°, and amino acid esters and l-ephedrine were obtained. Alanine and phenylglycine formed by hydrolysis of amino acid esters afforded R configuration with optical purity of 38% and 37%, respectively. The optical purity of l-ephedrine decreased only by 3.4% and 1.5% in several case during a cycle of the amino acid synthesis using l-ephedrine as a chiral reagent.抄録全体を表示PDF形式でダウンロード (627K) -
倉田 啓二, 山田 三和子, 粟屋 博義, 富永 義則, 松田 芳郎, 小林 五郎1978 年 98 巻 5 号 p. 623-630
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリー1, 9-Diazacycl [3.3.3] azine derivatives (XII, XIII) were synthesized by the reaction of acetic anhydride or ethoxymethylenemalononitrile with 1-imino-8-methyl-1H-pyrido-[1, 2-c] pyrimidine derivatives, which were obtained by the treatment of dimethyl cyanamidodithiocarboxylate or O-ethyl S-methyl cyanamidothiocarboxylate with 6-methyl-2-pyridineacetate derivatives. By the decarboxylation of XIII, 2-methylthio-1, 9-diazacycl [3.3.3] azine (XV), which was unstable as a free base, was obtained. On the other hand, 2, 3-dihydro-8-methyl-2-oxo-1, 9-diazacycl [3.3.3] azine hydrobromide (XVI) was obtained from the degradation of XVII. The nuclear magnetic resonance (NMR) spectral data suggested that XV may be a 12π-monocyclic antiaromatic compound.抄録全体を表示PDF形式でダウンロード (856K) -
倉田 啓二, 粟屋 博義, 富永 義則, 松田 芳郎, 小林 五郎1978 年 98 巻 5 号 p. 631-635
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリー1-Azaindolizine derivatives (Va, b, c) were easily obtained by the reaction of dimethyl N-(2-methylpyridin-5-yl) dithiocarbimidate (III) and α-halogenocarbonyl derivatives (ethyl bromoacetate, ω-bromoacetophenone, and ethyl bromocrotonate). 1-Azaindolizine derivatives (II, Va) were oxidized with perphthalic acid to afford 2-methylsulfonylimidazo-[1, 2-a] pyridine derivatives (VIa, b). Va was brominated with N-bromosuccinimide to ethyl 5-bromomethyl-2-methylthioimidazo [1, 2-a] pyridine-3-carboxylate (XII), which reacted with ammonia and methylamine to afford dihydrodiazacycl [3.2.3] azine derivatives (XIII, XIV).抄録全体を表示PDF形式でダウンロード (608K) -
小澤 貢, 森田 伸子, 馬場 きみ江, 秦 清之1978 年 98 巻 5 号 p. 636-638
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーA new dihydrofurocoumarin (IX) was isolated from the roots of Angelica keiskei KOIDZUMI (Umbelliferae), together with four known furocoumarins and two known dihydro-furocoumarins. The structure of IX was elucidated as 8 (S), 9 (R)-9-angeloyloxy-8, 9-dihydrooroselol.抄録全体を表示PDF形式でダウンロード (449K) -
加藤 百合子, 渡辺 富士雄1978 年 98 巻 5 号 p. 639-648
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe transition temperature and the heat of transition between three polymorphic forms of phenobarbital (form I, form II, and hydrate) were determined by various methods. Bioavailability of these three polymorphic forms was also evaluated by the in vivo absorption test. The transition temperature and the heat of transition were determined by the solubility measurement, the dissolution rate measurement, and differential scanning calorimetry. Crystalline energy differences were determined from the values of the heat of solution measured. The transition temperature and the heat of transition between form I and form II, and between hydrate and form II were determined to be 80.9°and 0.23 kcal/mol, and 49.1°and 1.52 kcal/mol, respectively, by the solubility measurement. These values agreed approximately with those obtained by other methods. On the other hand, the crystalline energy differences were in good agreement with those of the heat of transition by the solubility measurement. In the in vivo absorption test the plasma concentration versus time curves after oral administration of the three polymorphic forms of phenobarbital in rabbits were obtained. These results indicated that each polymorphic form was similar and these polymorphic states of phenobarbital do not affect its bioavailability.抄録全体を表示PDF形式でダウンロード (915K) -
田中 照夫, 早坂 鐵太郎, 斎藤 圀朗, 成田 仙一1978 年 98 巻 5 号 p. 649-652
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe reaction of 5, 6, 8, 9-tetrahydro-13bH-dibenzo [a, h] quinolizines with cyanogen bromide or ethyl chloroformate in the presence of magnesium oxide afforded a new ring system, 5, 6, 7, 8, 9, 14-hexahydrodibenz [d, g] azecines, in a good yield. By the application of this ring opening reaction, 2, 3, 11, 12-tetrahydroxy-5, 6, 7, 8, 9, 14-hexahydrodibenz [d, g]-azecine (5) was synthesized for pharmacological evaluation.抄録全体を表示PDF形式でダウンロード (615K) -
渡辺 裕司, 渡辺 和夫, 後藤 義明, 山口 正俊1978 年 98 巻 5 号 p. 653-659
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーIntracerebroventricular injection of penicillin G potassium (17.5, 35, 50, and 75μg) produced clonic convulsions, tonic flexor and extensor convulsions, and death due to respiratory embarassment in mice. The convulsion pattern was quite similar to that by peripherally administered picrotoxin, pentylenetetrazol (PTZ), or bemegride except strychnine which did not show marked tonic flexion. The tonic extension and death following penicillin increased in a dose-dependent manner. In order to clarify features of penicillin-induced convulsions, effect of various anticonvulsive drugs on penicillin-induced convulsions was compared with that on fits produced by PTZ or maximal electric shock (MES). Both the tonic extension and death induced by 50 μg of penicillin were prevented by the pretreatment with anticonvulsive drugs, phenytoin, phenobarbital, trimethadione, diazepam, or mephenesin, while chlorpromazine showed no anticonvulsive action. The penicillin-induced tonic extensor convulsion was, in general, more sensitive to anticonvulsive drugs than PTZ- or MES-induced convulsion. These results seem to suggest that penicillin-induced convulsion provides a useful tool for screening test of anticonvulsive actions of drugs.抄録全体を表示PDF形式でダウンロード (927K) -
三村 務, 大西 昇, 宮本 恵美子, 江川 宏, 青沼 繁1978 年 98 巻 5 号 p. 660-663
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーComparative examinations were made on palmitic acid, which has an anti-inflammatory effect, and myristic acid, which has no such effect, for their incorporation into various tissues and body fluids in intact and granuloma pouch rats by oral administration of 14C-labeled fatty acids. In intact rats, significantly higher radioactivity was found in the heart, liver, spleen, and adrenals 2 hr after administration of 1-14C-palmitic acid, compared to that in the group given 1-14C-myristic acid. This trend continued for 24 hr. In granuloma pouch-bearing rats, radioactivity showed a significantly higher distribution in the adrenals and pouch exudate 2 hr after 14C-palmitic acid administration, compared to the group given myristic acid. This tendency continued for 24 hr. However, radioactivity in the pouch wall showed higher distribution in the rats given 14C-myristic acid.抄録全体を表示PDF形式でダウンロード (583K) -
川野 タツ, 松村 瑛子1978 年 98 巻 5 号 p. 663-667
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe origin of a large amount of glycine in the hydrolyzate of the last feces excreted at the end of larval stage of silkworm was examined. Glycine produced by hydrolysis of the last feces of silkworm increased rapidly for about 8 days, first to 16.1 μmol/10 mg last feces, and then slowly to 19.5 μmol (approx. 65% of the total amino acids) for 20 days. On the other hand, 10 mg of the last feces contained 20.8μmol of uric acid, which produced glycine by hydrolysis under the same conditions as that of the last feces, and approx. 78 and 91% of uric acid was respectively converted into glycine during 8 and 20 days. Consequently, approx. 97% (18.9μmol/10 mg) of glycine in the hydrolyzate of the last feces may have been produced from uric acid, and the remainder (approx. 3%) from other compounds such as protein of mulberry leaves.抄録全体を表示PDF形式でダウンロード (650K) -
畠田 孝幸, 守 みどり, 中島 憲一郎, 吉村 実1978 年 98 巻 5 号 p. 668-672
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーThe dissociation constants (pK1, pK2) of 6-substituted thiouracils and uracils were determined by the spectrophotometric method. It was found that pK1 values of thiouracils were lower than those of the corresponding uracils. The effect of substituents in 6-position of these compounds was examined. Amino and phenyl groups, compared with alkyl group, decreases pK1 values. Further, the reaction of thiouracils with hydrogen peroxide was studied by the reaction kinetics. Thiouracils were finally converted to the corresponding uracils by hydrogen peroxide. Therefore, the first-order reaction constants were determined and the effect of substituents in 6-position of thiouracils was examined. The optimal experimental conditions were established for utilizing the above reaction to the quantitative determination of thiouracils.抄録全体を表示PDF形式でダウンロード (614K) -
沖川 正善, 二宮 義和, 羽坂 則子, 河野 信助, 上田 博之1978 年 98 巻 5 号 p. 672-675
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーIsolation of sandaracopimaric acid (III), 15-methyl agathate (IV), agatholic acid acetate (V), and agathalic acid (VI) from Manila copal is described. This is the first report on the isolation of agatholic acid acetate from a natural source.抄録全体を表示PDF形式でダウンロード (534K) -
渡辺 康, 佐野 倫男, 本橋 清, 高岸 靖, 土居 義男1978 年 98 巻 5 号 p. 676-678
発行日: 1978/05/25
公開日: 2008/05/30
ジャーナル フリーIn order to examine the effect of the amount of starch as a binder in the preparation of tablets on the bioavailability of drugs in humans, sulfamethoxazol tablets were prepared with the amount of starch varied from 5, 10, and 15%, and a mixed powder and fine granules prepared with the same composition as the tablets with 5% starch, and these five preparations were submitted to the dissolution test and measurement of sulfamethoxazol in serum after a single administration in healthy females. The dissolution rate tended to prolong with increasing amount of starch, but little difference was found in the area under blood concentration curve (AUC) of sulfamethoxazol by increase in the amount of starch. This difference in the in vitro and in vivo results was considered to be due to the rapid transition of the tablet into the intestines when administered on an empty stomach, and because the tablets are rapidly disintegrated and dissolved in the intestines by the use of a digestible starch, and because sulfamethoxazol dissolves easily at pH above 6.5. In the case of a mixed powder, maximum serum level of sulfamethoxazol was the lowest among all preparations, and the time to reach the maximum was also delayed. The reason for this was considered to be because moistening of the sulfa powder with water is rather poor in the mixed powder, the sulfa attaches on the stomach wall, becomes mixed with food, and its transition into the intestine is delayed. Such delay in reaching the maximum serum level was not observed in fine granules.抄録全体を表示PDF形式でダウンロード (476K)
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