巻号一覧
96 巻, 1 号
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気賀沢 和雄, 大谷 秀昭1976 年 96 巻 1 号 p. 1-5
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーDiphenylacetic acid esters of 2-diethylaminoethanol (I), 3-diethylaminopropanol (II), 4-diethylaminobutanol (III), 5-diethylaminopentanol (IV) and 6-diethylamino hexanol (V) were synthesized and the effect of the number of methylenes in the aminoalkyl esters on the rate of hydrolysis in an aqueous buffered solution was examined. Increase in the number of methylenes in the alkyl group of the aminoalkylesters decreased the hydrolysis rate constants in the alkaline side but not in the acidic side. In these series of compounds, there was a correlation between the observed pKa value and the logarithm of the hydrolysis rate constants (kOH). The esters containing a large number of methylenes were very stable and the formation of micelle was observed in aqueous solution.抄録全体を表示PDF形式でダウンロード (553K) -
気賀沢 和雄, 大谷 秀昭1976 年 96 巻 1 号 p. 6-11
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーThe diethylaminoethyl esters of ortho-, para- and di-substituted benzoic acid were synthesized and the effect of a substituent on the rate of hydrolysis in an aqueous buffer was examined. The hydrolysis rate constants were lower in the case of electron-releasing substituents and greater in the case of electron-attracting substituents in relatively higher pH solutions. There was a straight linear relationship between the Hammett substituent constant (σ) with the log (kOH/kOHo) values for the specific base-catalyzed hydrolysis of 2-diethylaminoethyl para-substituted benzoates (Fig. 4).抄録全体を表示PDF形式でダウンロード (562K) -
気賀沢 和雄, 大谷 秀昭1976 年 96 巻 1 号 p. 12-17
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーIn order to compare the rate of hydrolysis of the same aminoalkylesters of aromatic carboxylic acids with those of aliphatic carboxylic acids, 2-diethylaminoethyl esters of cyclohexanecarboxylic acid (I), cyclohexylacetic acid (II), phenylcyclohexylacetic acid (III), propionic acid (IV), capronic acid (V), and lauric acid (VI) were synthesized and the rate of their hydrolysis in an aqueous buffer solution was measured. The aliphatic esters such as I and II were generally unstable and the stable pH ranges were found to be on the alkaline side when compared with aromatic esters of the same type. It was found that the number of methylene in the straight chain of aliphatic esters such as IV, V and VI had almost no effect on the rate of hydrolysis.抄録全体を表示PDF形式でダウンロード (575K) -
中垣 正幸, 田川 美恵子1976 年 96 巻 1 号 p. 18-25
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーPeptization of ferric hydroxide by hydrochloric acid was examined. Precipitate of ferric hydroxide was added to an aqueous solution of hydrochloric acid and agitated for 30 min at 80° or boiled for 30 min. Efficiency of peptization was evaluated from the concentration of ferric hydroxide in the sol, which was determined by chelatometry after the colloidal particles had changed to ferric ion. It has been found that there is a maximum point of peptization at appropriate amount of ferric hydroxide precipitate added to hydrochloric acid. The degree of peptization increased with the amount of hydrogen ion adsorbed on the particle. The adsorption isotherm of hydrogen ion on the ferric hydroxide particle is well reproduced with Freundlich's equation. The minimum amount of hydrogen ion required to be adsorbed in order to peptize the particle (xmin) depends on ionic strength of the colloidal system (J), and the relation was experimentally determined as follows : xmin=0.95 √(J)+0.03 It has been concluded that hydrogen ion is responsible for peptization of ferric hydroxide as well as for stabilization of colloidal ferric hydroxide particles at about pH 2.5-5, while ferric ion cooperates with hydrogen ion to peptize and stabilize the sols at pH below 2.5.抄録全体を表示PDF形式でダウンロード (890K) -
竹田 正明1976 年 96 巻 1 号 p. 26-32
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーLocal anesthetic activites and other pharmacological actions of dl-cis-1-benzoyloxy-2-dimethylamino-1, 2, 3, 4-tetrahydronaphthalene (III) and its related compounds, including different types of chemical structures and stereoisomers, were examined. 1) The new series of compounds (I-VI) were found to have potent local anesthetic effect in guinea-pigs. Among them, III and a 4-aminobenzoloxy derivative (V) were more active than reference substances (procaine, lidocaine, and cocaine). 2) Introduction of an amino group into 4-position of the lipophilic benzoyloxy group of III intensified the local anesthetic activity. In IV, which is a trans-isomer of the cis-compound (III), positional interchange of benzoyloxy and dimethylamino groups on the tetraline ring resulted in complete loss of the activity. Accordingly, it was considered that the position of benzoyloxy and dimethylamino groups on the tetraline ring was of great importance for their local anesthetic activities. On the other hand, replacement of the ester group by ether group in III reduced the activity slightly. Another compound (VIII) substituted by phenyl group at 1-carbon atom of 2-diethylaminoethanol chain of procaine was more active than the original substance but less potent than the cyclic structured III. 3) Activity of the cis-form (III) exceeded that of the trans-isomer (IV) in corneal anesthesia. Similarly. dl-cis-1-benzoyloxy-2-dimethylaminoindane (I) was more potent than the corresponding trans-compound (II). 4) Highly significant relationship was found to exist between the intracutaneous anesthetic activity in guinea-pigs and the intravenous acute toxicity in mice for compounds I-V, VIII, procaine, lidocaine, and cocaine. However, no corrleation could be established between the anesthetic activity and the spasmolytic effect in isolated ileum of guinea-pigs.抄録全体を表示PDF形式でダウンロード (836K) -
吉田 桂, 乙益 寛隆1976 年 96 巻 1 号 p. 33-36
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリー2-Chloro-3-cyanopyridine compounds (2a, b), intermediates for the synthesis of thiamine were reacted with hydrazine hydrate to give the corresponding 1H-pyrazolo[3, 4-b]pyridine compounds (3a, b). The reaction of methyl 2-chloro-3-cyano-6-methylpyridine-4-carboxylate (5) with hydrazine hydrate afforded pyrido[3, 4-d]pyridazine compounds(6, 7). By refluxing with ethanol containing a small amount of H2SO4, 3-(ethoxycarbonylcyanomethylene)indolin-2(1H)-one was converted into ethyl 3-cyano-2-oxo-1, 2-dihydroquinoline-4-carboxylate(9). The reaction of hydrazine hydrate with 2-chloroderivative of (9) gave 1H-pyrazolo[3, 4-b]quino1ine compound (12).抄録全体を表示PDF形式でダウンロード (549K) -
飯田 武夫, 奥村 啓輔, 新井 良侑, 丹羽 正明, 伊藤 亮三, 伊藤 峰1976 年 96 巻 1 号 p. 37-43
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーThianaphthene, naphthalene, and their methyl homologues were identified from the cut 2 (boiling range 215 -250°) of the NTU Colorado shale oil. First, cut 2 was finely fedistilled into narrow subfractions of A, B, and C. After aliphatic hydrocarbons in the fraction A were removed by means of silica gel column chromatography, the concentrated thianaphthene and naphthalene mixture was separated by alumina column chromatography. It was found that naphthalene was adsorbed on alumina slightly more weakly than thianaphthene. Each of thianaphthene and naphthalene enriched fractions was purified by preparative gas chromatography, and these two compounds were identified with the authentic specimen by nuclear magnetic resonance, ultraviolet, and infrared spectra. Similarly, 6-methylthianaphthene, 1- and 2-methylnaphthene, and diphenyl were isolated from the fraction B and identified. Further, 2, 6- and 1, 6-dimethylnaphthalenes were identified in the fraction C.抄録全体を表示PDF形式でダウンロード (795K) -
小川 建志, 小野 行雄, 上田 陽1976 年 96 巻 1 号 p. 44-52
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーUltraviolet absorption spectra of 18 aldehyde azines, derived from two kinds of aromatic aldehydes, were measured in ethanol. All spectra were separated into their component peaks by the method of peak analysis. Results of peak analyses showed that the substituent at the para position of >C=N-N=CH-C6H5 group does not exert any rational substituent effect expected from their electronic nature. In order to clarify the nature of transition of absorption bands, theoretical transition energies of all compounds were calculated by the ASMO-SCF-LCAO -CI-MO method. The reasonable agreement between the experimental and theoretical transition energies of each compound indicate that almost all of component peaks are assignable to π-π* transition.抄録全体を表示PDF形式でダウンロード (796K) -
中田 泰浩, 三田 泰弘, 河野 重治1976 年 96 巻 1 号 p. 53-59
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーIn order to study photodegradation of vitamin K1, gas chromatographic determination of residual vitamin K1 in photodegradation products under aerobic or anaerobic condition was investigated, Quantitative analysis was carried out on the column packed with acidwashed and silanized Chromosorb W coated with 3% Silicone OV-1 at column temperature of 260°, and n-triacontane was used as an internal standard. It was possible to determine vitamin K1 without interference of photodegradation products under aerobic or anaerobic condition by the gas chromatography.抄録全体を表示PDF形式でダウンロード (733K) -
中垣 正幸, 宮田 堅司1976 年 96 巻 1 号 p. 60-65
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーEffect of the co-ion on the membrane permeability coefficient was studied theoretically and confirmed experimentally for cellulose membrane and for bovine lens capsule. When the mobility of the co-ion was much larger than that of the counter-ion, the reduced membrane permeability coefficient, Pγ, became larger than 1.0 and had a maximum value in the concentration range where the concentration of solution was almost equal to the charge density of the membrane. The permeability coefficient defined on the basis of the concentration gradient in the membrane, P*, and the diffusion potential, εD, in the membrane were estimated from experimental data. and also calculated theoretically. The agreement between experimental and theoretical values was good and values of both P* and εD increased in the same concentration range as Pγ became larger than 1.0 if the mobility of the co-ion was much larger than that of the counter-ion. It was concluded that, in the concentration range where the concentration of solution is almost equal to the charge density of the membrane, the reduced membrane permeability coefficient becomes larger than 1.0 and has a maximum value because the diffusion potential εD in the membrane has a maximum value and the the value of P* increases in this concentration range.抄録全体を表示PDF形式でダウンロード (694K) -
近 由喜子, 土橋 やよい, 桂 博二1976 年 96 巻 1 号 p. 66-70
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーA Hyphomycetes, strain F1, isolated from the excrements of Cettia diphone cantans was found to have the following characteristics on uricase production. 1) This strain was resistant to a high concentration of KCl or NaCl, and the addition of about 4.0% of these salts to the medium gave the maximum uricase production, which the was about two times in dry weight of the pellicle and about 15 times in the amount of enzyme compared to the normal fungal medium containing 0.05% of the salts. 2) The zinc-salt was found to be the only accelerator for the uricase production by this strain after detailed examination of various metal salts. Maximum uricase production was obtained by incubating this strain for 5 days in the medium containing 0.001-0.01 % of ZnSO4·7H2O or ZnCl2, when the amount of the enzyme was increased 3-4 fold compared to the absence of zinc salt.抄録全体を表示PDF形式でダウンロード (719K) -
稲垣 正博, 国吉 家治, 鍋田 三郎1976 年 96 巻 1 号 p. 71-74
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーCrystallization of DL-O-acetylpantolactone was carried out from a liquid of equimolar mixture of D- and L-O-acetylpantolactone by cooling at -10° to -20° for 5 days. From this crystallization process, it was found that the supercooled state of DL-O-acetylpantolactone was stable. The crystals obtained were confirmed to be a racemic cong1omerate by thermal analysis and infrared absorption spectrum. On the basis of these facts, the optical resolution of the crystals by seeded crystallization was examined in the binary system and successful results were obtained. As a result of the alternate D- and L-resolutions by this method, optical isomers were cbtained in 16% yield in a single cycle and their optical purity was over 80%.抄録全体を表示PDF形式でダウンロード (582K) -
下村 裕子, 栗山 悦子, 富沢 厚子1976 年 96 巻 1 号 p. 75-81
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーThe seedlings from Cannabis saliva L. seeds irradiated with different doses of γ-rays were examined, in order to determine the dose sufficient to kill the young plants naturally, before their hallucinnogenic component increases. The seeds of "Minamioshihara No.1", which were harvested in 1972 in Tochigi Prefecture, were irradiated with eight different doses of 60Coγ-rays on January 17, 1973, and the seedlings were examined sevefal times during subsequent 9 months, from March to November, 1973, and their morphological and histological effect were examined, and the results are summarized as follows : 1) Morphological Effects Samples irradiated with 1500 and 1000 krads developed radicles about 3 mm in length. Samples irradiated with 500, 200, and 50 krads grew into young plants with the first set of leaves, without lateral roots. Samples irradiated with 30 krads grew to about 10 cm high with a few lateral roots, and the epicotyls about 1 cm in length. These young plants from the irradiated seeds stayed in the same condition and then died. Samples irradiated with 15 and 5 krads grew in the same way as control until the stage of flowering. 2) Histological Effects Samples irradiated with 500, 200, 50, and 30 krads showed cell membranes of endodermis and pericycle to be partially lignified and suberized. The degree of changes was related to the dose of γ-rays. Samples irradiated with 30 krads showed withered cells near the end of the lateral nerves on the first and second sets of leaves. 3) Economical dose of 60Co γ-rays for inhibiting young plants from developing into adult ones was a minimum of 30 krads which made the young plants die. Irradiation with 50 krads of γ-rays will be required to kill the young plants completely before they develope hallucinogenic component.抄録全体を表示PDF形式でダウンロード (1611K) -
草野 源次郎, 村上 ゆり, 桜井 信子, 竹本 常松1976 年 96 巻 1 号 p. 82-85
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーDahurinol (I), dehydroxydahurinol (II), and isodahurinol (III) were isolated from the rhizome of Cimicifuga simplex WORMSK (Japanese name "Sarashinashoma"), while a new triterpene, 25-O-methylisodahurinol (IV), mp 237 -239°, C31H50O5, was isolated along with I and III from the rhizome of C. acerina (SIEB. et ZUCC.) C. Tanaka ("Ohbashoma"). The stereostructures of III and IV were established by the conversion of cimigenyl triacetate (XI), the total structure of which has already been elucidated, to isodahurinyl diacetate (VII) and of 25-O-methylcimigenyl monoacetate (XIII) to 25-O-methylisodahurinyldiacetate (VIII).抄録全体を表示PDF形式でダウンロード (667K) -
磯野 博, 立浪 節子, 黒野 吾市1976 年 96 巻 1 号 p. 86-90
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーAliphatic compounds were fractionated from a few fresh plants by anion-exchange resin column chromatography, using nonaqueous media, and qualitatively and quantitatively determined by gas-liquid chromatography. The plants examined were leaves of Allium schoenoprasum L., Hosta undlata B., Ophiopogon japonicus K., and Hemerocallis fulva L., and stems of Scilla japonica B. All of them were found to contain aldehydes, mainly octacosanal, triacontanal, and dotriacontanal. By this method, fatty acid methyl esters were found in the stems of Scilla japonica B. and the leaves of Hosta undlata B.Allium schoenoprasum L. contained 16-hentriacontanone in the leaves.抄録全体を表示PDF形式でダウンロード (567K) -
小澤 光, 池田 實, 豊口 義夫1976 年 96 巻 1 号 p. 91-98
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーPharmacological interactions among noosteroidal antiinflammatory drugs were studied by determining their hypothermic action and acute toxicity in mice, and their antipyretic action in adjuvant-induced fever rats. 1) The hypothermic actions of the combined use of naproxen with aminopyrine (a), indomethacin with aminopyrine (b), and phenylbutazone with aminopyrine (c) in mice were additive. 2) The antipyretic action of (a) in adjuvant-induced fever rats was additive. 3) The acute toxicities of (a), (b), and (c) were found to be partially antagonistic or antagonistic by estimation according to the diagram proposed by Guddum. 4) The safety indices of the analgesic actions of (a), (b), and (c) were calculated on the basis of 50% analgesic effective dose and 50% lethal dose. The index values of (a), (b), and (c) were 49.6, 11.1, and 5.8, respectively. These and previous results suggested that the combined use of aminopyrine, a weak basic drug, with some weak acidic nonsteroidal anti-inflammatory drugs (e.g. naproxen) was benefrcial.抄録全体を表示PDF形式でダウンロード (901K) -
中西 美智夫, 大江 孝範, 鶴田 峯生, 松尾 浩, 桜木 俊治, 丸山 裕1976 年 96 巻 1 号 p. 99-109
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーA series of xanthenyl- and benzopyranopyridinylacetic acid derivatives were synthesized by various methods, and the relationship between their structure and anti-inflammatory activity was assayed by the method of ultraviolet erythema. It was thereby found that 2-(5H-[1]benzopyrano[2, 3-b]pyridin-7-yl)propionic acid (IV-2) had the most potent anti-inflammatory activity.抄録全体を表示PDF形式でダウンロード (1011K) -
大塚 昭信, 柿内 千枝子1976 年 96 巻 1 号 p. 110-115
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーThe flocculation-deflocculation behavior of chloramphenicol (CP) in aqueous solutions of poly(vinylpyrrolidone) (PVP) and ionic surfactant mixture was studied by the measurement of sedimentation, adsorption, and ζ potential. In the presence of PVP, the addition of a small amount of sodium dodecyl sulfate (SDS) produced a deflocculated state which showed a remarkable decrease in sedimentation volume. Taking into consideration that the interaction of PVP with SDS takes place significantly, it can be thought, from the adsorption and the ζ potential data, that CP particles were deflocculated by both the steric and electrical effects produced by the adsorption of the PVP-SDS complex. With further increase in the concentration of SDS the adsorption of PVP was reduced and the suspension was converted into a flocculated state. In the series of PVP/dodecylammonium chloride (DACl) system, it was likely that PVP and DA+ were adsorbed competitively. The addition of DACl with a sufficient amount of PVP caused deflocculation. On the other hand, the effect of dodecylammonium thiocyanate (DASCN) upon suspensions was not remarkable in spite of the larger adsorption of DA+ than in the DACl-PVP system. The sedimentation volume was kept large over the range of DASCN concentration below c.m.c. even in the presence of PVP. This can be attributed to the fact that DA+ binds to PVP with the aid of SCN-, leading to a decrease in hydrophilic property of adsorbed PVP.抄録全体を表示PDF形式でダウンロード (748K) -
三宅 康夫, 豊島 昭二, 竹中 英雄1976 年 96 巻 1 号 p. 116-121
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーRelationship between compacting progress of pharmaceutical powder and measurement variation of apparent density in the case of compacting phenomenon by means of tapping and compacting phenomenon in course of mixing with 1% calcium stearate was examined. At the beginning of compacting of a powder, measurement variation of apparent density decreased with progress of compacting, and their relationship was shown by experimental equation (1). σN/ρN×100=κ1 log △εN+κ2(1) where N is progress of compacting, i.e., number of tapping or cumulative revolution of the mixer, ρN is the mean value of measured apparent density, σN is standard deviation, △εN is differential change of porosity between compacting progress N and N+1, and κ1 and κ2 are experimental constants. After a certain degree of compacting progress, σN/ρN×100 did not decrease with decrease of log △εN, but became constant. This was considered to be an unavoidal experimental error. σN/ρN×100=κ3 (2) Experimental constant κ3 was thought to change according to the apparatus for measurement, powder, and other conditions. Equation (2) did not apply when abnormal phenomenon, such as segregation of particles in tapping, was likely to occur.抄録全体を表示PDF形式でダウンロード (737K) -
小川 俊太郎, 吉田 昭義, 三谷 洋子1976 年 96 巻 1 号 p. 122-124
発行日: 1976/01/25
公開日: 2008/05/30
ジャーナル フリーA method was established for the quantitative determination of glycyrrhizin in Glycyrrhiza radix by high-speed liquid chromatography. Glycyrrhizin is separated in approximately 13 min using a 1 m Permaphase AAX column with a mobile phase of 30% isopropanol in phosphate buffer (pH 5.2) at 50°. It was concluded by comparison of this method with the three currently used methods (thin-layer chromatography, diethylaminoethyl-cellulose and gas-liquid chromatography methods) that this method was significantly better than other methods with respect to simplicity, analytical time, and accuracy.抄録全体を表示PDF形式でダウンロード (453K)
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