巻号一覧
25 巻, 12 号
選択された号の論文の52件中1～50を表示しています
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岩瀬 廣, 村井 朝夫1977 年 25 巻 12 号 p. 3129-3136
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーhe fragmentation of five derivatives of isobutylamine, 3-methylthiopropylamine, β-phenylethylamine, tyramine and dopamine upon electron impact is studied for the concurrent ultramicrodetermination and the selective identification of amines by mass fragmentography. The results obtained in this study indicated that trimethylsilyl derivative was the most preferable for the concurrent ultramicrodetermination of amines because this derivative produced the common intense ion at m/e 174, which is specific for amines. Using mass fragmentography monitored at m/e 174, about 10-11g of amine can be detected.抄録全体を表示PDF形式でダウンロード (727K) -
辻川 輝昭, 立田 元視1977 年 25 巻 12 号 p. 3137-3146
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーUnder a nitrogen atmosphere, anti-isomers of 2-benzylidenehydrazinopyrimidines underwent isomerization easily to their syn-isomers by irradiation with ultraviolet light in a benzene solution, but in the presence of oxygen, photosensitized auto-oxidation occurred to afford 3-aryl-1, 2, 4-triazolo [4, 3-a] pyrimidines. When irradiated in the same manner, 2-benzylidenehydrazino-1, 3, 5-triazine derivatives decomposed into benzaldehydes and 2-hydroxy-1, 3, 5-triazines.抄録全体を表示PDF形式でダウンロード (918K) -
辻川 輝昭, 林 正教1977 年 25 巻 12 号 p. 3147-3154
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーIn hope of antihypertensive activity, 2-(2-tetrahydrothienyl)-3-hydroxy-5, 5-dimethyl-2-cyclohexen-1-one (3) was synthesized by the routes of either (A) on heating a mixture of dimedone (7) and 2-chlorotetrahydrothiophene or (B) by the coupling of 7 with 2, 3-dihydrothiophene (9) in the presence of acid. Several related compounds were also prepared.抄録全体を表示PDF形式でダウンロード (905K) -
村上 篤司, 赤堀 幸男1977 年 25 巻 12 号 p. 3155-3162
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーA physicochemical and mathematical model of the mechanism of physiological action was assumed, and the model was applied on prostaglandins. A conformation-action relationship was studied using the model, and high values of correlation coefficients were obtained. Biological activities of prostaglandins on rat uterus, guinea pig ileum, and rabbit jejunum were explained using the model. Active sites of prostaglandins were derived from the mathematical model. They are the oxygen atom bonded to the carbon atom C1, the oxygen atom bonded to C9, the oxygen atom bonded to C15, and the carbon atom C5 or C20.抄録全体を表示PDF形式でダウンロード (859K) -
小嶋 仲夫, 杉浦 幸雄, 田中 久1977 年 25 巻 12 号 p. 3163-3171
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe interaction between the indium complexes and human serum proteins has been investigated by electrophoresis and gel filtration. Excess indium above serum transferrin level bound to albumin and α1-globulins besides to transferrin. The sulfhydryl-containing ligands and ethylenediaminetetraacetic acid (EDTA) prevented the indium binding by albumin, in contrast with common amino acids. The indium complexes of penicillamine, 2, 3-dithiopropanol (BAL), and EDTA resist the transfer of indium from the complexes to transferrin and the ability is related to the stability of the complexes, and to the molecular form and size of the ligands. Thioglycolic acid which prevents the hydrolysis of indium and forms the indium-transferrin-thioglycolate ternary complex, is available for the effective preparation of 113mIn-or 111In-transferrin. The binding-affinity of In (III) to ovotransferrin was approximately equal to that of Fe (III). The indium complex of EDTA was present in the form of the dimer at the physiological pH, as well as the ferric complex. On the basis of these results, the usefulness of the inert indium complexes of EDTA, penicillamine, BAL, and the disulfhydryl-containing peptides as imaging agents, has been discussed.抄録全体を表示PDF形式でダウンロード (1058K) -
杉浦 衛, 山田 隆, 磯部 正和1977 年 25 巻 12 号 p. 3172-3176
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe thermal inactivationoof the semi-alkaline proteinase from Aspergillus melleus, proceeded following the first order kinetics. The activation energy for the thermal inactivation was calculated to be 53 kcal per mol. Autolysis takes place directly proportional with the inactivation and the enzyme was degraded into oligopeptide and or amino acid. It was found that calcium ion, ammonium sulfate, glycerol and saccharose have a stabilizing effect on the semi-alkaline proteinase against the thermal inactivation. In the enzyme, 4-6 mol of calcium ion per mol of protein were found to bound, and by the loss of calcium ion, the enzyme became extremely unstable. In the presence of denaturing agents such as urea, guanidine-HCl and alcohols, the inactivation of the enzyme was accelerated and proceeded with first order kinetics. Activation energy for thermal inactivation decreased in the presence of urea and guanidine-HCl, but unchanged in the presence of alcohols. From these results, it was concluded that thermal inactivation of the semi-alkaline proteinase proceeded in two steps, that is, denaturation with conformational change and followed degradation with the residual proteinase. The rate limiting step was the denaturation.抄録全体を表示PDF形式でダウンロード (662K) -
佐々木 喜男, 藤原 英明, 川木 秀子, 岡崎 雄交1977 年 25 巻 12 号 p. 3177-3181
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe 1 : 1 complex formations between pyridine bases and Eu (DPM)3 are approved at equimolar, excess base and excess Eu (DPM)3 conditions. The equilibrium constants and complex shifts are estimated by the graphic and simulation methods of the observed results of the above three conditions. The complex shifts thus obtained showed good correspondence with infinite concent-ration shifts and the so-called S values. The equilibrium constants are solvent dependent, whereas the complex shifts are not.抄録全体を表示PDF形式でダウンロード (542K) -
草野 源次郎, 北条 祥子, 近藤 嘉和, 竹本 常松1977 年 25 巻 12 号 p. 3182-3189
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーCimicifugoside (I), mp 237-238°, C37H54O<<11> was isolated along with friedelin, β-sitosterol, β-sitosteryl glucoside, 25-O-methylcimigenol, cimigenol and cimigenyl xyloside from the roots of Cimicifuga simplex. The structure (I) was proposed for cimicifugoside on the basis of chemical and physicochemical data. The major topic is chemistry of a hydrolysis product, cimicifugenin A (IV) and its derivatives.抄録全体を表示PDF形式でダウンロード (1016K) -
亀井 敏夫, 鈴木 肇, 松崎 明紀, 大谷 敏夫, 近藤 久雄, 中村 昭四郎1977 年 25 巻 12 号 p. 3190-3197
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーCholesterol esterase was purified from the culture filtrate of Streptomyces lavendulae by a procedure involving precipitation with ammonium sulfate and acetone, gel filtration on Sepharose CL-4B, and rechromatography on Sepharose CL-4B after treatment of Triton X-100. The purified enzyme was detected as a single band by polyacrylamide disc electrophoresis, while one main band and three minor bands were observed by SDS gel electrophoresis. The molecular weight of the main band was 29000. The enzyme was inhibited by Hg2+, Ag+ and DFP. Long-chain fatty acid esters of cholesterol were hydrolyzed preferentially and pH optimum was 6.0. This enzyme could be used to the determination of total serum cholesterol with cholesterol oxidase from Streptomyces violascens.抄録全体を表示PDF形式でダウンロード (946K) -
青野 哲也, 岸本 彰二, 荒木 義昭, 野口 俊作1977 年 25 巻 12 号 p. 3198-3209
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe relative reactivity in each position of 1-indancarboxylic acid (IV) toward electro-hilic substitution reaction such as chlorination, bromination, acylation, sulfonation and nitration was examined and it was found that the 6-position is the most reactive. By these reactions, pharmacologically interesting meta-substituted phenylacetic acid derivatives were readily obtained. Electrophilic chlorination of IV followed by cycloalkylation provided an improved alternative synthetic method of antiinflammatory 6-chloro-5-cyclohexyl-1-indancarboxylic acid (TAI-284, I) and its analogs.抄録全体を表示PDF形式でダウンロード (1370K) -
沢田 洋介, 中野 史朗, 谷山 兵三1977 年 25 巻 12 号 p. 3210-3217
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリー1. Streptomyces lavendulae ISP-5069 produces racemomycin-A which yields β-lysine as a component on hydrolysis. β-Lysine was derived from an intermediate α, ε-diaminopimelic acid via lysine pathway. Exogenous lysine acted as a donor of β-lysine to form racemomycin-C and-B by S. lavendulae NT-1008 by means of incorporation of 14C-labeled lysine. 2. Two taxonomically different strains, S. lavendulae NT-1008 and S. albidoflavus S-0003, were selected as the strains producing racemomycin-A, -C, and-B as a mixture. These antibiotics were present both in the intracellular pool and in the broth. 3. Addition of 14C-racemomycin-A to the culture medium resulted in the incorporation of 14C into racemomycin-C and-B. Majority of the radioactivity was present in the extracellular racemomycin-C and-B, but a significant portion was present in the intracellular antibiotics. These data indicate that racemomycin-C and-B were transformed stepwisely from racemomycin-A and β-lysine, suggesting an endogenous formation.抄録全体を表示PDF形式でダウンロード (980K) -
高村 喜代子, 伊藤 みずほ1977 年 25 巻 12 号 p. 3218-3225
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーEffects of metal ions and flavonoids on the oxidatio of ascorbic acid (I) have been investigated polarographically in the acetate buffer solution of pH 5.4. since I gives a diffusion-controlled anodic wave due to a two-electron oxidation to form dehydroascorbic acid, the rate of the oxidation of I can be followed by measuring the change in the limiting current of I with time. The rate of the oxidation of I was enhanced by the presence of some metal ions. Among them, the effect of copper (II) was especially pronounced. Such the fact can be explained on the basis of the formation of a coordinative linkage between metal and ascorbate ions and the reducibility of metal ions. Contrary to this, flavonoids exhibited an inhibition effect on the copper (II)-catalyzed oxidation of I. The effect became more marked in the order of 3-hydroxyflavone<rutin<quercetin, but no inhibition was observed for flavone. From the experimental result that the complex forming tendency of copper (II) with flavonoids increase in the order of flavone<3-hydroxyflavone<rutin<quercetin, a decrease in the concentration of free copper (II) as a result of the complex formation between flavonoids and copper (II), was found to be primarily responsible for the inhibition effect of flavonoids.抄録全体を表示PDF形式でダウンロード (828K) -
井上 隆夫, 藤田 正雄1977 年 25 巻 12 号 p. 3226-3231
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリー^<14>C-Labelled isoliquiritigenin was efficiently incorporated into puerarin of Pueraria lobata but 14C-labelled daidzein was almost not into it. These results support that the C-glycosylation occurs at the stage of chalcone or flavanone. Further competitive feeding experiments with T-or 14C-labelled isoliquiritigenin and liquiritigenin suggest that Cglycosylchalcone would be a possible intermediate for the biosynthesis of puerarin.抄録全体を表示PDF形式でダウンロード (757K) -
城武 昇一, 坂口 武一1977 年 25 巻 12 号 p. 3232-3238
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーA new cytosinium copper chloride complex was synthesized from diluted hydrochloric acid solution. The site of copper ion being coordinated with cytosine was examined by means of infrared and selective broadening in proton magnetic resonance (PMR) spectrum. On the basis of these data, it was suggested that copper ion is coordinated with the C(2)=O of cytosine, and that composition of the cytosinium copper chloride complex is 4 : 1 ratio of ligand to metal. On the basis of infrared and PMR spectral studies, it was suggested that the N(3)site of cytosine is strongly bound to proton rather than to copper ion under an acid condition.抄録全体を表示PDF形式でダウンロード (765K) -
山次 信幸, 須田 恭子, 尾上 泰子, 加藤 元彦1977 年 25 巻 12 号 p. 3239-3246
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーTreatment of 2-substituted 1, N6-etheno-c-AMP (c-AMP : adenosine 3', 5'-cyclic phosphate) derivatives with N-bromosuccinimide (NBS) under mild conditions gave the corresponding 2-substituted-c-AMP. Therefore, the route (c-AMP→1, N6-etheno-c-AMP→2-substituted 1, N6-etheno-c-AMP→2-substituted c-AMP) offers an excellent way to synthesize the last compound from c-AMP. The yields of this deblocking reaction of the etheno group were increased by the adjustment of the solution to alkaline after bromination. The probable reaction mechanism involving the bromination and the subsequent hydrolysis has been proposed.抄録全体を表示PDF形式でダウンロード (859K) -
宮寺 哲男, 川野 洋一, 畠 忠, 田村 千尋, 太刀川 隆治1977 年 25 巻 12 号 p. 3247-3254
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThree 1, 4-benzodiazepine N-oxides, diazepam N-oxide (IIIa), nordiazepam N-oxide (IIIb) and chlordiazepoxide (IV) were submitted to 1, 3-dipolar cycloaddition reaction with dimethyl acetylenedicarboxylate to give quinoxaline derivatives (Va from IIIa ; Vb from IIIb ; XI and XII from IV). It is likely that the cycloaddition reactions involve the rearrangement of Beckmann type in which initially formed adducts (i.e., VIa) rearrange to quinoxaline derivatives (i.e., VIIa). The structural determination of XII was made by X-ray crystallographic analysis.抄録全体を表示PDF形式でダウンロード (923K) -
中山 妙子, 中嶋 暉躬, 曽我部 博文1977 年 25 巻 12 号 p. 3255-3260
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThree kinds of snake angiotensins have been isolated from the incubation product of snake (Elaphe climocophora) kidney extract with homologous plasma. The amino acid sequences were deduced by dansyl method as follows : Asp-Arg-Val-Tyr-Val-His-Pro-Phe X-Asx-Arg-Val-Tyr-Val-His-Pro-Phe-Tyr X-Asx-Arg-Val-Tyr-Val-His-Pro-Phe-Tyr-Leu Tyrosine in position 9 was different from histidine of mammalian angiotensins or serine of the fowl. Position 5 was valine as in so-called bovine angiotensin.抄録全体を表示PDF形式でダウンロード (741K) -
植松 正吾, 赤堀 幸男1977 年 25 巻 12 号 p. 3261-3269
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe tautomerism of 5-fluorobenzofuroxan was studied by the proton magnetic resonance at 60 and 100 MHz. The rate of intramolecular rearrangement between 5-fluorobenzofuroxan (ABCX) and 6-fluorobenzofuroxan (A'B'C'X') was obtained by analyzing the line shapes of proton magnetic resonance signals. The theoretical spectra were calculated by means of a computer program based on the density matrix theory of the nonmutual exchange developed by Johnson, and the theoretical spectra showed a good agreement with the experimental line shapes in the temperature range from -78°to +30°. Activation parameters for the intramolecular rearrangement were found to be ⊿H&nedot;=5∼10kcal/mol and ⊿S&nedot;=-33∼-17 cal/deg·mol.抄録全体を表示PDF形式でダウンロード (850K) -
松田 工, 本庄 紀子, 山崎 企善, 後藤 良宣1977 年 25 巻 12 号 p. 3270-3276
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of 2, 5-diarylthiazole 3-oxides (IIa-e) with acetic anhydride was studied. The intermediates of this reaction, 4, 5-diacetoxy-2, 5-diaryl-4, 5-dihydrothiazoles (Va-1-Ve-1, Va-2-Ve-2), were isolated and their structures were determined by their chemical behavior and spectral data.抄録全体を表示PDF形式でダウンロード (744K) -
笠井 良次, 松浦 清子, 田中 治, 真田 修一, 庄司 順三1977 年 25 巻 12 号 p. 3277-3282
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーComplete trimethylsilylation of 20 (S)-protopanaxadiol (11), 20 (S)-protopanaxatriol (12) (Ginseng-sapogenins) and dammarenediol-II (13) was furnished by the action of trimethylsilylimidazole. The mass spectra of the pertrimethylsilyl ethers of 11, 12, and 13 (TMSi-11, -12, and -13) exhibited characteristic fragmentations around their C-20, which were diagnostic for structure determination of triterpenes of this type. The mass spectra of TMSi-ethers of the deuterated compounds of 11 (11-d2 and -d5) demonstrated that no 1, 2-elimination of TMSiOH at C-3 and -12 was involved in the fragmentation. With reference to the reports of the mass spectrometry of TMSi-oligosaccharides, the mass spectra of Ginseng saponins (ginsenosides-Rb1 (1), -Rb2 (2), -Rc (3), -Rd (4), -Re (5), -Rf (6), -Rg1 (7), and -Rg2 (8) were also studied, the results of which were found to be useful for identification and structure determination of oligoglycosides of this type.抄録全体を表示PDF形式でダウンロード (638K) -
藤本 貞毅, 中川 力, 小原 晃1977 年 25 巻 12 号 p. 3283-3288
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe properties of the acid phosphatase isolated in a homogeneous state from soybean (Glycine max) have been investigated in detail. The enzyme catalyzed the hydrolysis of a wide variety of phospholylated compounds including phosphomonoesters, nucleotide mono-, di-and triphosphate, and inorganic pyrophosphate. No activity was detected for nicotinamide adenine dinucleotide and diphenyl phosphate. The enzyme activity was inhibited by orthophosphate, arsenate, fluoride, molybdate, and heavy metal ions including Cu2+, Zn2+, Hg2+ and Ag+. Treatment of the enzyme with chelating agents, reducing agents and oxidizing agents resulted in inactivation of the enzyme. The reduction of the absorbance at 540 nm of the enzyme was observed in parallel with the loss of the enzyme activity by the treatment with ethylenediaminetetraacetic acid and rongalit, but not with H2O2. The enzyme had a molecular weight of approximately 240000. Polyacrylamide disc gel electrophoresis in the presence of sodium dodecyl sulfate suggested that the enzyme dissociated into subunits with molecular weight of approximately 60000. The amino acid and carbohydrate composition of the enzyme were also determined.抄録全体を表示PDF形式でダウンロード (642K) -
三宅 昭夫, 栗木 久, 伊藤 克巳, 西川 正夫, 岡 良和1977 年 25 巻 12 号 p. 3289-3300
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーIn a search for a new type of β-adrenoceptor agonist, a series of N, N'-disubstituted 2, 5-diamino-6-hydroxy-1, 2, 3, 4-tetrahydro-1-naphthalenols (2a-q), in which the 5-hydroxyl group of the previously reported rigid catecholamine (1) was replaced by methylamino, dimethylamino, ethylamino, dimethylamino, methanesulfonylamino, ureido, and formamido groups, were synthesized from 6-benzyloxy-5-nitro-4, 3-dihydro-1 (2H)-naphthalenone (6). 5-Chloro-2-isopropylamino derivative (53) was also prepared using an intermediate of those syntheses. Biological results for the two derivatives (2d and 2e) are presented.抄録全体を表示PDF形式でダウンロード (1327K) -
伊藤 一男, 田中 斉1977 年 25 巻 12 号 p. 3301-3305
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーReaction of erysodienol (4) with methyl iodide afforded the corresponding dibenzazonine (7), whose structure was confirmed by identification with the authentic specimen, prepared by N-methylation of a known secondary amine (1). On the other hand, erysodienone methiodide (6), synthesized by N-methylation of erysodienone (3), was treated with alkali reagents in methanol and ethanol to yield dibenzazonines (8 and 9), which have newly formed methoxyl and ethoxyl groups at C5-position in dibenzazonine skeleton.抄録全体を表示PDF形式でダウンロード (631K) -
水谷 彰, 松下 芳広, 水谷 隆治1977 年 25 巻 12 号 p. 3306-3311
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーOne of two hypocalcemic substances from the bovine thymus (TP1) was investigated. As a material for purification, it was confirmed by chromatography on diethylaminoethylcellulose that the fraction precipitated at 0-15% ammonium sulfate concentration was better than the 0-20% precipitate. Molecular weight of TP1 was 66000 by sedimentation equilibrium and this result agreed with that obtained by sodium dodecyl sulfate polyacrylamide gel electrophoresis (68000) and suggested that TP1 was not composed of subunit. The circular dichroism spectrum of TP1 showed that the contents of α-helix, β-structure, and random form were 7, 39 and 54%, respectively. TP1 contained 2.07 mol of the sulfhydryl residues by the mercury orange method. By the treatment at 56°for 30 min, hypocalcemic activity disappeared and the activity also disappeared by the treatment at 37°for 1 hr in acidic (pH 1.4) or alkaline (pH 12.6) solutions.抄録全体を表示PDF形式でダウンロード (728K) -
小林 茂, 木原 勝, 志津 暁, 片山 定, 池田 治吉, 北広 和雄, 松本 宏1977 年 25 巻 12 号 p. 3312-3323
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe apogalanthamine analogs, 10, 11-methylenedioxy-, 10, 11-dimethoxy-, and 11, 12-dimethoxy-5, 6, 7, 8-tetrahydrodibenz [c, e] azocines (2, 5, and 7, respectively) and their N-substituted derivatives (1, 3, 4, 6, 8, and 9) as α-adrenergic blocking agents, and the related compounds, 2, 3-dimethoxy-, 2, 3-methylenedioxy-, and 11-methoxy-5, 6, 7, 8-tetrahydrodibenz [c, e] azocines (10, 11, and 12, respectively) were synthesized by intramolecular cyclization of the corresponding amino-alcohols (30a-f) via the corresponding bromo-amines (16a-f). The preparation of the nitrovinyl compounds (19a-f) as startnig materials for the amino-alcohols was investigated. The conformation of these azocines was discussed in relation to nuclear magnetic resonance spectral data.抄録全体を表示PDF形式でダウンロード (1189K) -
宮崎 利夫, 及川 直子, 山田 陽城1977 年 25 巻 12 号 p. 3324-3328
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーWater-soluble polysaccharide from ascocarps of Cordyceps sinensis was purified by ethanol fractionation and gel filtration. Purified polysaccharide, CS-I, [α] D-45.3°(c=1, H2O), gave D-galactose (phenylosazone, mp 185-187°) and D-mannose (phenyl-hydrazone, mp 199-200°) in a molar ratio of 1 : 1 by acid hydrolysis. From the results of periodate oxidation, Smith-type degradation, methylation analysis, partial acid hydrolysis, and 13C-NMR spectrometry, it is concluded that CS-I is a highly branched galactomannan which consists of mannan core and galactosyl oligomer containing branches. The mannan core mainly contains (1→2)-α-linked-D-mannopyranosyl residues, and the branches contain (1→3), (1→5), and (1→6)-linked-D-galactofuranosyl, (1→4)-linked-D-galactopyranosyl residues. The non-reducing ends are D-galactofuranose and D-manno-pyranose, and the branching points are D-mannopyranosyl residues.抄録全体を表示PDF形式でダウンロード (653K) -
前田 満和, 尾川 修, 川添 豊1977 年 25 巻 12 号 p. 3329-3333
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーVarious classes of aliphatic amines including amino acids were catalytically deuterated in D2O in the presence of Adams platinum at 30°and 100°. The positions deuterated depended on the chemical structure of the amino nitrogen ; α-hydrogens were the most stable in primary amines, while they were the most labile in tertiary amines. The reaction profile of secondary amines seems to be intermediate between those of primary and tertiary amines. Quaternary amines did not react under the reaction condition studied. A tentative reaction mechanism was proposed.抄録全体を表示PDF形式でダウンロード (592K) -
山中 宏, 阿部 弘之, 坂本 尚夫1977 年 25 巻 12 号 p. 3334-3339
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーBenzoylation of 2, 4-dimethyl-(Ia), 2, 4, 6-trimethyl-pyrimidine (Ib), 2, 4-dimethyl-quinazoline (Ic), 2, 4-dimethyl-(Id), 2, 4, 6-trimethyl-pyridine (Ie), and 2, 4-dimethyl-quinoline (If) with ethyl benzoate under basic conditions were performed. In analogy with the nitrosation with ethyl nitrite, methyl groups on the 4-position of IIa-f were preferentially benzoylated to give 4-phenacyl derivatives. Structures of all the products were determined by chemical derivatization.抄録全体を表示PDF形式でダウンロード (786K) -
仲井 由宣, 福岡 英平, 中島 新一郎, 山本 恵司1977 年 25 巻 12 号 p. 3340-3346
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーCrystalline medicinals were ground with microcrystalline cellulose by a stainless steel shaker mill. The medicinal changed in their physical properties in grinding the mixture of a 10% medicinal. X-ray reflection lines due to the medicinal decreased in their intensities with the increasing time of grinding. The intensity of characteristic lines was not observed after the 2 hr grinding and halo pattern was obtained. The heat of fusion due to the medicinals was not observed for the 2 hr ground mixture. There was the critical content of medicinals in the ground mixture to show the halo pattern on the X-ray diffractogram and no heat of fusion on the thermogram. The medicinals were released rapidly from the ground mixtures in the aqueous solution and the solution reached the saturated concentration in a very short time. These phenomena occurred in all crystalline medicinals independent of the molecular properties, such as structure, size, and polarity. The residual cellulose, the ground mixture of benzoic acid from which the acid had been released, had the large pore volume of capillaries at about 30-40 A. It was estimated that the medicinal molecules were dispersed within the cellulose as a molecule or a microassembly of the molecules having no preferred orientation. The assembly was probably isolated being enclosed by the cellulose molecules which were bound by hydrogen bond. The ground mixture may be regarded as an"entropy frozen solution, "that is, a medicinal dissolves in cellulose without the ability of molecular translation movement.抄録全体を表示PDF形式でダウンロード (825K) -
東 常政, 磯野 清1977 年 25 巻 12 号 p. 3347-3353
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーTransglycosylation from acylated pyrimidine nucleoside to purines was originally developed by Miyaki, et al. To apply this method to the naturally occurring pyrimidine nucleosides having a labile sugar moiety, we studied the improvement of this reaction. As model compounds, tri-O-acetyl-3-benzoyluridine (1) and tetraacetylcytidine (2) were employed. Reaction conditions and yields were greatly improved by utilizing (1) trimethylsilyl derivatives of exo-N-acylpurines as a glycosyl acceptor, (2) trimethylsilyl trifluoromethanesulfonate as a catalyst in acetonitrile-dichloroethane. Because of the mild reaction conditions and high yield, this procedure may be regarded as a versatile method for transglycosylation, which was shown by the successful preparation of purine analogs of the polyoxin and octosyl acid nucleosides having labile amino-or anhydrosugar uronic acid.抄録全体を表示PDF形式でダウンロード (861K) -
平尾 健一, 海野 重視, 三浦 偉俊, 米光 宰1977 年 25 巻 12 号 p. 3354-3359
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe photochemical behavior of tricyclo [5. 2. 2. 02, 6] undeca-3, 10-dien-9-one ring system (4), which was prepared by Diels-Alder reaction of cyclohexadienone derivatives and cyclopentadiene, has been studied under triplet sensitization and direct irradiation. In the triplet state, this ring system undergoes the oxa-di-π-methane (ODPM) rearrangement, while the 1, 3-acyl migration occurs from the singlet state. The triplet energy was estimated to be between 70 and 72 kcal/mol on the basis of sensitization by various sensitizers.抄録全体を表示PDF形式でダウンロード (712K) -
坂本 正徳, 宮沢 恭子, 富松 祥郎1977 年 25 巻 12 号 p. 3360-3365
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーReaction of several conjugated C-N double bond compounds with diketene was carried out with a view to establishing the structure-reactivity relationship of the 1, 3-diaza-1, 3-butadiene system. Formamidine derivatives (IIIa-h) reacted with diketene in benzene to form the products (Va-h) through 1, 4-dipolar cycloaddition with the elimination of dimethylamine, respectively. Similarly, reaction of diketene with 2-(p-dimethylaminobenzylideneamino) benzothiazole (IXa) and 2-(p-dimethylaminobenzylideneamino) benzimidazole (IXb) respectively afforded 3-acetyl-2-(p-dimethylaminophenyl)-2, 3-dihydro-4-oxo-4H-pyrimido [2, 1-b] benzothiazole (Xa) and 3-acetyl-2-(p-dimethylaminophenyl)-2, 3-dihydro-4-oxo-4H-pyrimido-[1, 2-a] benzimidazole (Xb).抄録全体を表示PDF形式でダウンロード (664K) -
東 昇, 有村 博文, 石川 英之1977 年 25 巻 12 号 p. 3366-3369
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーAn apprehension for virus contaminant cannot be completely eliminated from urokinase (plasminogen activator) preparation originated from human urine theoretically. In this experiment the effect of heat-treatment of urokinase at 60°for 10 hr on infectivity of viruses added intentionally to urokinase samples was investigated. (1) Ten kinds of viruses used were completely inactivated within 5 hr of incubation at 60°. (2) Decrease of urokinase activity due to heat-treatment was avoided by adding albumin as a stabilizer.抄録全体を表示PDF形式でダウンロード (467K) -
沢田 誠吾, 宮坂 貞, 荒川 基一1977 年 25 巻 12 号 p. 3370-3375
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーSeventeen 3-(substituted-phenyl) thiazolo [2, 3-b] benzothiazolium perchlorates (3) were synthesized by acid-cyclization of the ketosulfides (2), which were prepared by alkylation of 2-mercaptobenzothiazole sodium salt with substituted phenacyl halides (1). Some of the phenacyl halides were prepared by chloroacetylation of substituted benzenes, and the others by bromination of the corresponding substituted acetophenones.抄録全体を表示PDF形式でダウンロード (706K) -
青山 敏信, 前田 共秀, 堀岡 正義1977 年 25 巻 12 号 p. 3376-3380
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーEffect of humidity and water content on the degradation of propantheline bromide mixed with dried aluminum hydroxide gel was examined. Degradation of propantheline bromide in this system is accelerated with increasingly higher humidity until under 75% RH and decreased under more high humidity, and was the most marked when 0.2 ml of water was added per 5 g of the mixture. Degradation became slower as the amount of water added became greater or smaller than that. Addition of 0.2 ml/5 g of water means that water molecule forms a monolayer on the surface of dried aluminum hydroxide gel. Since the gel used orginally contained 4% of water, addition of 0.2 ml/5 g means that two layers of water molecule were formed on the surface of the gel. Degradation of propantheline bromide is most marked when water molecule forms a monolayer to several layers on the surface of the gel. This degradation was assumed to be initiated through the layer on the surface of dried aluminum hydroxide gel.抄録全体を表示PDF形式でダウンロード (628K) -
松尾 光芳, 田原 吉幸1977 年 25 巻 12 号 p. 3381-3384
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーHigh performance liquid chromatography was employed to rapidly separate tocopherols and their model compounds, chroman-6-ols. Good separation of these compounds was obtained. By use of naphthalene as an internal standard, tocopherol was exactly quantitated in the range from 0.3 to 3.0 μg. Tocopherols and a model compound dispersed in a cell culture medium were analysed with ease.抄録全体を表示PDF形式でダウンロード (552K) -
伊藤 敬一, 駒木 玲子, 関屋 実1977 年 25 巻 12 号 p. 3385-3388
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーAs N-functionalized derivatives of amino acids [chemical formula] N-alkylthiomethyl (X=RS) and N-amidomethyl (X=RCONH) derivatives have been furnished by the reaction among XH, formaldehyde, and amino acid.抄録全体を表示PDF形式でダウンロード (547K) -
高荷 昌子, 中野 真知子, 高橋 幸太郎1977 年 25 巻 12 号 p. 3388-3390
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリー(+)-Catechin-7β-D-glucopyranoside was isolated from the wooden part of Schizandra nigra MAX抄録全体を表示PDF形式でダウンロード (486K) -
永松 国助, 城戸 靖雅, 浦久保 五郎1977 年 25 巻 12 号 p. 3390-3394
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーA sensitive and specific method of radioimmunoassay for 2, 5-dimethoxy-4-methylamphetamine (DOM) was developed, using anti-DOM antiserum obtained by immunizing guinea pig with DOM-glutaraldehyde-HSA conjugate and 125I-N-succinyl-DOM-tyrosine methylester (125I-DOM) as a labeled hapten. DOM, 125I-DOM and antibody came up to equilibrium over 15 hours at 4°of the incubation time in the radioimmunoassay system at pH 7.4 in phosphate buffer. Bound 125I-DOM was precipitated with satd. (NH4)2SO4 and the radioactivity of the bound labeled hapten was determined by γ-counting. The displacement curve was linear when the percentage binding of 125I-DOM was plotted against logarithmic increase of unlabeled DOM from 1 to 100 ng. The antiserum showed less affinity for various phenylisopropylamine derivatives and biogenic amines and there was no interfering substance in a normal serum.抄録全体を表示PDF形式でダウンロード (551K) -
中西 進 /, ELWOOD V. JENSEN1977 年 25 巻 12 号 p. 3395-3397
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of fluorinated steroidal enamines with perchloryl fluoride furnished 2, 2-difluoro-and 2, 2, 4α-trifluorinated steroids. Changes in infrared absorption frequency due to the introduction of fluorine are discussed.抄録全体を表示PDF形式でダウンロード (472K) -
中西 進 /, ELWOOD V. JENSEN1977 年 25 巻 12 号 p. 3398-3400
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーSteroid alcohols are converted to their chloroformate esters by reaction with phosgene in the presence of a base. Replacement of chlorine by fluorine takes place smoothly by treatment with anhydrous thallous fluoride in ethylene glycol dimethyl ether. Significant shifts in the positions of both infrared spectra-carbonyl and carbon-oxygen single bond absorption frequency due to the fluorine are discussed.抄録全体を表示PDF形式でダウンロード (472K) -
今村 順茂, 一番ケ瀬 尚1977 年 25 巻 12 号 p. 3400-3405
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーEffect of plasma-protein binding displacement on the intestinal absorption of sulfonamides in rabbits was investigated by using salicylic acid and phenylbutazone as displacing drugs. Salicylic acid and phenylbutazone significantly reduced the in situ intestinal absorption of sulfadimethoxine that showed high binding to plasma proteins. These two displacing drugs also enhanced the in situ intestinal exsorption of sulfadimethoxine. However, salicylic acid and phenylbutazone showed no significant effect in the transport of sulfadimethoxine from mucosal to serosal side solution through the intestinal membrane or the uptake of sulfadimethoxine by the intestinal preparation in vitro. In addition, salicylic acid and phenylbutazone did not affect the in situ intestinal absorption and exsorption of sulfanilamide that showed little binding to plasma proteins. From these results, it is concluded that the displacement of one drug from its plasma-protein binding sites by another drug is an important determinant affecting drug absorption.抄録全体を表示PDF形式でダウンロード (756K) -
亀谷 富士夫, 須見 泰子1977 年 25 巻 12 号 p. 3405-3408
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーBinding affinities of five 4-substituted benzenesulfonyl propylureas to bovine serum albumin (BSA) were investigated by equilibrium dialysis method. Those of chlorpropamide (CPU) to BSA was also investigated by dynamic dialysis method using 35S labelled CPU. Results of both methods agreed very well. Binding paramethers of these compounds to BSA were obtained assuming that there were two classes of binding sites. CPU and 4-iodobenzenesulfonyl propylurea were bound to BSA stronger than benzenesulfonyl, p-toluenesulfonyl and 4-aminobenzenesulfonyl propylureas with regard to the primary binding site.抄録全体を表示PDF形式でダウンロード (548K) -
吉崎 正雄, 富森 毅, 難波 恒雄1977 年 25 巻 12 号 p. 3408-3409
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーSix flavonoids ; luteolin-7-glucoside, isoquercitrin, vitexin, isovitexin, orientin, and homo-orientin were isolated from the leaves of Gleditsia japonica MIQUEL and G. sinensis LAMARCK.抄録全体を表示PDF形式でダウンロード (408K) -
中村 泰子, 太田 稔, 上野 芳夫1977 年 25 巻 12 号 p. 3410-3414
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーInteraction of the 12, 13-epoxytrichothecenes and related mycotoxins with epoxide hydrolase and glutathione-S-transferase (GSH-S-transferase) from rat liver was examined in vitro. Neither hydrolysis of safrole oxide by the microsomal epoxide hydrolase nor conjugation of 2, 3-epoxy-(p-nitrophenoxy) propane with GSH by the soluble GSH-S-transferase was interfered with the trichothecenes such as T-2 toxin and fusarenon-X. Gas-liquid chromatography (GLC) analysis and colorimetric determination of the residual GSH revealed that the trichothecenes were inert to the partially purified GSH-S-transferase. In contrast to the trichothecenes, PR-toxin, an epoxide mycotoxin from Penicillium roqueforti, and lactones such as patulin and penicillic acid from Penicillium and Aspergillus spp., were found to react non-enzymatically with GSH in molar ratio of 1 : 1.抄録全体を表示PDF形式でダウンロード (594K) -
南原 利夫, 池川 繁男, 石田 秀樹, 細田 宏1977 年 25 巻 12 号 p. 3415-3418
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーThe stereochemistry of the hydrogen addition at C-4 in the microbial 5α-hydrogenation of a ⊿4-3-ketosteroid has been investigated. 4-d1-4-Androstene-3, 17-dione was converted by incubation with Penicillium decumbens into 5α-androstane-3, 17-dione. The position of deuterium retained in the product was elucidated to be 4α by 1H nuclear magnetic resonance spectroscopy using the lanthanide shift reagent. These results led to the conclusion that the hydrogen addition at C-4 occurs stereospecifically from the β-side in this biotransformation.抄録全体を表示PDF形式でダウンロード (561K) -
大森 秀信, 植田 千裕, 枡井 雅一郎1977 年 25 巻 12 号 p. 3419-3422
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーElectronic spectra of twenty four α-cyanobenzylideneanilines (I) were measured in ethanol. The effects of substituents on the spectra suggested that the electronic interaction of the two phenyl rings in I is stronger than that in the corresponding benzylideneanilines owing to the electron-withdrawing effect of the α-cyano group.抄録全体を表示PDF形式でダウンロード (549K) -
阿部 フミ子, 岡部 光, 山内 辰郎1977 年 25 巻 12 号 p. 3422-3424
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーCerbinal, yellow pigment having iridoid skeletal with Δ3, 5, 7, 9 (1)-tetraene, and 10-formyl and 11-carbomethoxy residues, was isolated along with 10-carboxy-(cerberic acid) and 11-carboxy-(cerberinic acid) derivatives from the bark of Cerbera manghas L.抄録全体を表示PDF形式でダウンロード (468K) -
崎谷 陽子, 花野 学, 宮内 芳子, 酒井 浩子1977 年 25 巻 12 号 p. 3425-3432
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーA study was made by the in situ recirculating perfusion technique as to the effect of urea (0.1, 0.5, 1.0M) on the absorption of salicylic acid, benzoic acid and aminopyrine in rat intestinal tract. The addition of 0.5 or 1.0M urea resulted in increased drug permeability of the gill of gold fish, while that of 1.0M urea significantly decreased intestinal drug absorption clearance. With urea added to a perfusate, its osmotic pressure was elevated and the water flux from the intestine to the blood was decreased. A significant correlationship existed with a positive regression coefficient between water flux and clearance. Similarly, both water flux and clearance were reduced by adding NaCl so as to give the same tonicity as 1.0M urea. This effect was not significantly different from that of adding 1.0M urea. From these observations it is concluded that urea has no such effect in rat intestines as is observed in gold fish.抄録全体を表示PDF形式でダウンロード (940K) -
杉林 堅次, 森本 雍憲, 灘井 種一, 加藤 好夫1977 年 25 巻 12 号 p. 3433-3434
発行日: 1977/12/25
公開日: 2008/03/31
ジャーナル フリーAfter intravenous injection in mice, 5-fluorouracil-6-3H entrapped in albumin microspheres localized mainly in the liver, and the disappearance rate of radioactivity in microspheres from the tissue was very slow in comparison with that of free drug. Such preferential localization and sustained release of entrapped drugs suggested that albumin microspheres are useful as drug-carrier in chemotherapy.抄録全体を表示PDF形式でダウンロード (397K)