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Volume 20, Issue 4
Displaying 1-46 of 46 articles from this issue
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SENKICHI NAGASAKI, NOBUHIKO NAKAZAWA, YASUAKI OSADA, TAKESHI HASHIZUME ...1972 Volume 20 Issue 4 Pages 639-649
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe antibacterial activities of 64 naphthyridine derivatives were tested. Ultimately, potassium 1, 4-dihydro-1-methyl-7-[2-(5-nitro-2-furyl) vinyl]-4-oxo-1, 8 -naphthyridine-3-carboxylate (677K) was selected as the most active compound. Compound 677K exhibited excellent antibacterial activities against either gram-positive or gram-negative bacteria in vitro. Furthermore, 677K exhibited high activities against experimental infection of streptococci, diplococci, or staphylococci in mice when administered orally. The activity on diplococcal infection in mice was higher than that of aminobenzylpenicillin, tetracycline, chloramphenicol, sulfisomezole, and dihydroxymethylfuratrizine. The effect of 677K against experimental typhosis was small. Cross resistance was seen between 677K and DF, but not between 677K and NA.View full abstractDownload PDF (3539K) -
HARUO KITAGAWA, MITSUKAZU KITADA, TOHRU HORIE1972 Volume 20 Issue 4 Pages 650-656
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSN-Demethylation of ρ-substituted dimethylaniline derivatives, N-methyl-N-alkylaniline derivatives and N-methyl-N-acylaniline derivatives was investigated. The rates of N-demethylation of several series of ρ-substituted dimethylaniline depended upon their lipid solubilities. The more lipid soluble the amine was, the more readily it was demethylated. The ρ-substituted dimethylanilines of high lipid solubilities revealed small Km and Ks values, whereas those of low lipid solubilities exhibited large Km and Ks values. N-Demethylation activity of the high lipid soluble ρ-substituted dimethylaniline was intensely stimulated by phenobarbital administration in comparison with that of the low lipid soluble p-substituted dimethylaniline. N-Demethylation of ρ-substituted dimethylaniline of low lipid solubility was inhibited more strongly than that of high lipid solubility by SKF 525-A, but this relation between lipid solubility and inhibitory rate was not observed in carbon monoxide inhibition. The studies on N-demethylation of N-methyl-N-alkylaniline derivatives revealed that the rate of N-demethylation did not always depend on the lipid solubilities of amines. It was suggested that steric hindrance about the nitrogen atom interfered with N-demethylation of N-methyl-N-alkylaniline derivatives. In the studies on N-demethylation of N-methyl-N-acylaniline derivatives, the difference of N-demethylation rate between N-methyl-N-propyonylaniline and N-methyl-N-benzoylaniline seemed to depend on the spectral change per P-450 rather than lipid solubility.View full abstractDownload PDF (1000K) -
GORO KOBAYASHI, YOSHIRO MATSUDA, REIKO NATSUKI, MASAKATSU SONE1972 Volume 20 Issue 4 Pages 657-663
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReaction of 3, 4-dihydroisoquinolineacetonitrile (I) and methyl 1-cyano-2, 2-dimethylthioacrylate (II) gave 3-cyano-2-methylthio-4-oxo-6, 7-dihydrobenzo [α] quinolizines (III). III reacted with various amines to form 1, 3-dicyano-2-amino-4-oxo-6, 7-dihydrobenzo-[α] quinolizines (IVa-g). III also reacted with active methylene compounds to form 1, 3-dicyano-4-oxo-6, 7-dihydrobenzo [α] quinolizines (V-IX).
In the reaction of 1, 3-dicyano-2-methylthio-4-oxo-6, 7-dihydrobenzo [α] quinolizines (IIIna) and 2-amino-1, 3-dicyano-4-oxo-6, 7-dihydrobenzo [α] quinolizine (IVd) with concentrated sulfuric acid, the cyano group in 1-position was found to be easily liberated and that in 3-position was converted into a carboxamide group.
Reduction of 1, 3-dicyano-4-oxo-6, 7-dihydrobenzo [α] quinolizines (IIIa, b, IVa, Vb) with sodium borohydride in ethanol or N, N-dimethylformamide gave 1, 3-dicyano-4-oxo-1, 6, 7, 11b-tetrahydro-9, 10-dimetoxybenzo [α] quinolizines (XI, XIIa, b, XIII) by the reduction of quinolizine skeleton.View full abstractDownload PDF (919K) -
MASUMI ITOH1972 Volume 20 Issue 4 Pages 664-668
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSA novel amino-activation by the carbamate formation of amino acids and peptides in aqueous solution are described. The coupling reaction of acylamino acid active esters with carbamates is several times faster than with corresponding amine components.View full abstractDownload PDF (787K) -
TAISUKE MATSUO, TAKUICHI MIKI1972 Volume 20 Issue 4 Pages 669-676
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe Diels-Alder reaction of 5-ethoxy-4-ethoxycarbonylmethyloxazole (I) with dienophiles was investigated. The stereochemistry of the addition products that had an exocyclic double bond was confirmed by the spectroscopic data. The reaction of I with maleic anhydride gave endo-(II) and exo-adduct (III), and the isomerization of II to 1II proceeded easily. The reaction of I with eight symmetrical dienophiles afforded the isomeric adducts. Similar treatment of asymmetrical dienophiles afforded the corresponding adducts, respectively. The stereochemistry of these adducts was discussed.View full abstractDownload PDF (1373K) -
MAMORU KAMIYA, YUKIO AKAHORI1972 Volume 20 Issue 4 Pages 677-681
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe semiempirical SC F-MO-CI calculations were performed with the aid of the variable β-core procedure for a systematic investigation of the π-electronic structures and spectra of a series of pyrones and coumarins including sulfur derivatives. The calculated results on the π-π* transitions indicated several significant effects of the heteroatom replacement upon the polarization direction and oscillator strength. The calculated values of the singlet π-π* transition energies for the compounds excepting the thiothia-derivatives and the polarization directions of the lowest two π-π* transitions of coumarins and so on were found to be in good agreement with the observed results. Also, the changes in the π-electronic distribution in going from the ground to the lowest 1 (π, π*) and/or 3 (π, π*) state were in good correlation with a few experimental facts.View full abstractDownload PDF (741K) -
SHUN-ICHI NAITO, SEIMEI OSUMI, KYOKO SEKISHIRO, MICHIKO HIROSE1972 Volume 20 Issue 4 Pages 682-688
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSPlasma levels of trimetazidine in rabbits, rats, and mice were determined. Plasma levels in animals showed unusual curve about 1 hr after oral administration and this reason was investigated by determining distribution of the drug in animal tissues and excretion of the drug in bile.
Metabolic pathways of trimetazidine in rabbits were investigated qualitatively and it was ascertained by thin-layer chromatography that the methylene group connecting the benzene and piperazine rings is not severed by metabolism in rabbits.View full abstractDownload PDF (1053K) -
YASUO INUBUSHI, TAKASHI HARAYAMA, KENJUN TAKESHIMA1972 Volume 20 Issue 4 Pages 689-693
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe trans(IVa) and cis (IVb) isomers of 7, 8-dimethoxy-N-methyl-2-phenyl-1, 2, 4, 5-tetrahydro-3H-3-benzazepin-1-ol were stereospecifically synthesized.View full abstractDownload PDF (905K) -
SHIGERU KOBAYASHI, KANJI KITAMURA, AKIRA MIURA, MIYOKO FUKUDA, MASARU ...1972 Volume 20 Issue 4 Pages 694-699
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe reaction product of diphenide (I) with potassium cyanide, previously described as 2'-cyanomethy1-2-biphenylcarboxylic acid (II), is in fact a phenanthrol derivative (V). The acid (II) is an intermediate in the reaction. These facts were provedby synthesis of II from I by an alternative, unambiguous method. In the last step of the synthesis, only boron tribromide is effective for hydrolysis of the ester (IX). This is the first time it has been employed as a hydrolyzing agent for an ester.
In contrast to previous results, 9-phenanthrol (III) was found to be a product of the calcium salt of V.View full abstractDownload PDF (1198K) -
TSUNETOSHI KAITO, KOJI KASUYA1972 Volume 20 Issue 4 Pages 700-707
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSImidazoline was benzoylated with 3, 5-dinitrobenzoyl chloride and sodium carbonate buffer by the usual Schotten-Baumann reaction to develop a deep red color. The reaction was carried out in the dark and the solution after addition of 3, 5-dinitrobenzoyl chloride to imidazoline was immediately brought to a slightly acidic or neutral pH by which the color developed. This coloration was applied for the determination of naphazoline in pharmaceuticals and the mechanism of this reaction was also investigated.View full abstractDownload PDF (1175K) -
KIICHIRO KAKEMI, HITOSHI SEZAKI, SHOZO MURANISHI, HIROYASU OGATA, SATO ...1972 Volume 20 Issue 4 Pages 708-714
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSMechanism of the absorption of drugs from oil in water emulsions was studied in the rat large intestine. Synthesized esters of fatty acids and phthalic acid-0.1% Polysorbate 80 was chosen as the emulsion system, the oil/water volume ratio was varied from 0 to 1, and the absorption from emulsions of sulfapyridine, salicylamide, and of acetanilide was investigated using in situ recirculation and loop techniques.
In the absorption of drugs having partition coefficients of larger than one, amount of drugs in aqueous phase rather than their concentrations was a critical factor for the absorption from oil in water emulsions.
In the absorption of poorly oil-soluble drugs, drug absorption from emulsions was larger than the one from aqueous solutions when the overall volume of emulsions was kept constant, which suggested the importance of absolute volume of aqueous phase in the absorption of drugs from such systems.
Usually drugs dissolved in oil were absorbed mainly via aqueous phase.View full abstractDownload PDF (2549K) -
KIICHIRO KAKEMI, HITOSHI SEZAKI, SHOZO MURANISHI, HIROYASU OGATA, KUMI ...1972 Volume 20 Issue 4 Pages 715-720
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDrug absorption from oily solutions was investigated by the rat large intestine using in situ re circulation technique. Three model drugs (acetanilide, sulfapyridine, and salicylamide) and three different kinds of oil (isopropyl palmitate, ethyl laurate, and diethyl phthalate) were chosen for absorption studies.
It was found that in oily solution, drug absorption through the large intestinal membrane usually took place after being liberated from oil into the secreting fluid.
In the absorption of a drug having oil/water partition coefficient of less than one, apparent enhancement in the absorption was observed. This was attributed to the small volume of secreting fluid (aqueous phase) and the local concentration build-up of a drug at the absorptive surface.
Some comparisons have been made with the absorptive behavior of drugs from oil in water emulsions.View full abstractDownload PDF (906K) -
SANYA AKABOSHI, MIKIO SHIKITA, EIICHI MATSUI, HIROSUKE HOSHINO1972 Volume 20 Issue 4 Pages 721-724
Published: April 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSCysteine ethyl ester hydrochloride was as effective as cysteine in saving the life of X-irradiated (600 R) mice, regardless of whether it was given orally or intraperitoneally. However, the compound did not prolong the life of the animals who received higher dose (800 R) of X-rays.Notwithstanding rather weak effectiveness in radiation protection, cysteine ethyl ester will be useful because of its low toxicity; median lethal oral dose in mice was 35.8 mmoles/kg, while the radioprotective effect was observable in an oral dose of 2.0 mmoles/kg.View full abstractDownload PDF (559K) -
YOSHIHISA OKAMOTO, ATSUSHI TAKADA, TAKEO UEDA1972 Volume 20 Issue 4 Pages 725-729
Published: April 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSThe reactions of ethyl ω-haloalkylimidate hydrochloride, X-(CH2) n-C(=NH) OEt HCl, where X is Cl or Br and n is 1 or 3, with aminoheterocycles are described.The reaction course might be affected by the number of n in the imidate employed for this reaction. Each structure of the reaction products was confirmed by the data on the nuclear magnetic resonance spectrum, the infrared spectra and the mass-analyses.View full abstractDownload PDF (823K) -
NAOKATA MORITA, MASAMI SHIMOKORIYAMA, MINEO SHIMIZU, MUNEHISA ARISAWA1972 Volume 20 Issue 4 Pages 730-733
Published: April 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSBesides tectroridin, two components, one of which is novel, have now been isolated from n-butanol extract of the rhizome of Iris tectorum MAXIMOWICZ.The one (I), mp 210-214°, colorless microneedles, was idetntified as androsin (acetovanillon-β-D-glucoside). The other (IIA) C23H24O12, mp 212-214°, was assumed to be 5, 7, 3'-trihydroxy-6, 4'-dimethoxyisofiavone-7-β-D-glucoside. We proposed the names iristectorin A and iristectrorigenin A for the glycoside and its aglycone, respectively.View full abstractDownload PDF (754K) -
OSAMU IRINO, MITSURU TATEISHI, CHIEKO MIURA, KAZUNAGA FUKAWA1972 Volume 20 Issue 4 Pages 734-740
Published: April 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSThe metabolites of IA (2-indanamine hydrochloride) have been investigated in rats and rabbits. When IA (100mg/kg) was administered to rats, following metabolites were found together with unchanged IA:cis-, trans-1-hydroxy-2-indanamine, cis-, trans-1, 2-indandiol, 5-hydroxy-2-indanamine. In the urine of rabbits dosed 100mg/kg of IA, the presence of 2-indanol precursors of 2-indanone and was recognized together with the above metabolites. From the investigation about the sequence of metabolites of IA, it became evident that the oxidative deamination of IA was only occurred in rabbits, but not in rats.View full abstractDownload PDF (1273K) -
MASAO MURAYAMA, EISUKE SETO, TAKASHI OKUBO, IWAO MORITA, ITSUO DOBASHI ...1972 Volume 20 Issue 4 Pages 741-746
Published: April 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSAlternative syntheses of Suberosin (V) as well as Osthol (I) have been described. When the metal salts of 2-hydroxy-4-methoxybenzaldehyde (XI), such as Li, Na, K, Ca and Ti salt, were treated with γ, γ-dimethylallyl bromide in benzene and water, the four compounds, 3-γ, γ-dimethylallyl-2-hydroxy-4-methoxybenzaldehyde (IV), 5-γ, γ-dimethylally1- 2-hydroxy-4-methoxybenzaldehyde (VIII), 2-γ, γ-dimethylallyloxy-4-methoxybenzaldehyde (IX) and 2-γ, γ-dimethylallyl-5-methoxyphenol (X) were obtained.
Furthermore, IX was converted to VIII by the thermal rearrangement of the γ, γ-dimethylallyl group.View full abstractDownload PDF (942K) -
YOSHIFUMI MAKI, MASAHIRO TAKAYA1972 Volume 20 Issue 4 Pages 747-750
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSUpon treatment of 2-phenyl-4, 5-dichloro-3 (2H)-pyridazinone (I) with sodium alkoxides, a ring contraction product, 1-phenyl-4-alkoxy-5-alkoxycarbonylpyrazole (III), was obtained as a major product. From the available data, a mechanism for the ring contraction was proposed. A most interesting finding is that formation of III does not involve an anomalous substitution as has been observed in the ring contraction of I to 1-phenyl-3-hydroxypyrazole-5-carboxylic acid (II) upon treatment with aqueous sodium hydroxide.View full abstractDownload PDF (670K) -
SHOICHI NAKAJIMA, YOSHIKO KOIKE, SHIGEKO KATO1972 Volume 20 Issue 4 Pages 751-754
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSMethylanhydroitaconitin was synthesized from 4-(2-methoxy-4-methylphenyl)-3-butenoic acid, which was derived from 2-methoxy-4-methylbenzaldehyde by heating with sodium succinate and acetic anhydride. The difference, of temperature in the latter reaction caused the formation of 1, 4-bis (2-methoxy-4-methylphenyl)-1, 3-butadiene. Methylstyrylmaleic anhydride was also prepared.View full abstractDownload PDF (653K) -
KOICHIRO KAWASHIMA, EUN BANG LEE, TOSHIKI HIRAI, KOJI TAKEUCHI, KEIJIR ...1972 Volume 20 Issue 4 Pages 755-758
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSEffects of crude platycodin on gastric secretion and experimental ulcerations were studied in the rat. Crude platycodin markedly inhibited gastric secretion and prevented peptic ulcers in the pylorus ligated rat but had a rather slight effect on stress induced ulceration. Curative effect of crude platycodin (25mg/kg/day) on acetic acid induced ulceration was also observed.View full abstractDownload PDF (700K) -
KAZUHIRO IMAI, MOTOTAKA SUGIURA, HIROAKI KUBO, ZENZO TAMURA, KAZUMI OH ...1972 Volume 20 Issue 4 Pages 759-764
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSOne gram of L-DOPA was administered orally to the patients with Parkinson's disease and normal persons. Plasma DOPA and catecholamines, urinary DOPA, catecholamines and aromatic acids were determined by gas chromatography both before and after acid hydrolysis. DOPA and dopamine conjugate were detected in the plasma soon after the administration, while large personal deviations were observed both in their concentration and time courses. During 24 hr, 0.53%, 4.24%, 32.0%, and 25.9% in average of the administered L-DOPA were excreted in urine as DOPA, dopamine, DOPAC and HVA respectively in a free and conjugated form.View full abstractDownload PDF (937K) -
HIROSHI TERADA1972 Volume 20 Issue 4 Pages 765-771
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe partition behaviors of amphoteric acids with pH were examined based on the theoretical considerations. The apparent partition coefficient, defined as the ratio of the activities of the acid in organic and aqueous phases, is maximal at the isoelectric point. When pK1, is much smaller than pK2, the apparent partition coefficient coincides with the true partition coefficient, defined as the ratio of the activities of the neutralform of the acid in the two phases, at this point. The former changes linearly with slopesof +1 and-1 in the region of pK1>>pH and pK2<<pH. By applying the method of Ang when the presence of the zwitter-ionic form can be excluded, it was demonstrated that the true partition coefficient can be determined exactly from this pH-partition curve, even if the ionization constants of the acid are not known. This method also gives the values of the two ionization constants, so it seemed to be available for determination of the ionization constants of acids, which are very slightly soluble in water.
The partition coefficients of p-aminobenzoic acid, sulfonamide and sulfamonomethoxine were measured in an n-octanol/H2O system at 25°over a wide pH range. The variation of the partition coefficients with pH confirmed the above considerations well. The values obtained for the true partition coefficients and ionization constants agreed well with the results of others.View full abstractDownload PDF (991K) -
TAKEO HIGASHINO, MITSUO UCHIDA, EISAKU HAYASHI1972 Volume 20 Issue 4 Pages 772-777
Published: April 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSMass spectra of 4-substituted pyrido [2, 3-d] pyrimidines were examined.
Fragmentations of pyrido [2, 3-d] pyrimidine (I), 4 (3H)-pyrido [2, 3-d] pyrimidinone (VIII), 4-chloropyrido [2, 3-d] pyrimidine (IX) and 4-methoxypyrido [2, 3-d] pyrimidine (X) were analogous to those of corresponding quinazoline derivatives, respectively. Fragmentation of 4-methylpyrido [2, 3-d] pyrimidine (II) afforded (M-·H)+ intermediate written as diazatropylium ion 3' in pathway leading to [M-(·H+CHE≡CH)]+ ion 4. 4-Ethylpyrido [2, 3-d] pyrimidine (III), 4-phenylpyrido [2, 3-d] pyrimidine (V) and 4-phenyl-3, 4-dihydropyrido [2, 3-d] pyrimidine (VI) gave intermediate written as cyclic flagment ion (8, 12, 16) as same as shown in fragmentation of 2-ethylquinoline and 1-ethylisoquinoline. In any way the predominant fragmentation of 4-substituted pyrido [2, 3-d] pyrimidines was proceeded by consecutive loss of cyano radical and hydrogen cyanide accompanied with breakdown or migration of the substituent.View full abstractDownload PDF (751K) -
MASASHI TOMODA, MASAYO UNO1972 Volume 20 Issue 4 Pages 778-782
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSPlantasan, the seed mucilage of Plantago major L.var.asiatica DECAISNE, has been subjected to Smith degradation.The polysaccharide obtained as the degradation product was an arabinoxylan, and the molar ratio of D-xylose: L-arabinose was 9: 1.After methanolysis, the O-methyl derivatives characterised from the methylated polysaccharide were methyl glycosides of 2, 3, 5-trimethyl L-arabinose, 2, 3-dinaethyl D-xylose and 3-methyl D-xylose. As the result of these investigations and periodate oxidation, a possible structure of the arabinoxylan is proposed.In addition to this polysaccharide, glycerol, glycolaldehyde, ethylene glycol, D-xylose, L-arabinose and their glycosides were determined as Smith degradation products obtained from plantasan.View full abstractDownload PDF (762K) -
YOSHIO ARATA, TOMIKO SHIODA1972 Volume 20 Issue 4 Pages 783-788
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReaction of di (10-octahydroquinolizinyl) hydroxylamine (I) with methyl iodide in methanol gave 6-hydroxyimino-1-methyldecahydroazecine methiodide (II), 5-methyl-10-methoxyoctahydroquinolizinium iodide (III) and 3, 4, 6, 7, 8, 9-hexahydro-2H-qunolizine (IV). Reduction of II with lithium in liquid ammonia afforded 6-hydroxyimino-1-methyldecahydroazecine (X), 6-amino-1-methyloctahydroazecine (XI) and IV. In addition, the similar reduction of III led to the formation of IV, VIII and cis-1-methyl-1, 2, 3, 4, 7, 8, 9, 10-octahydroazecine (XIV).View full abstractDownload PDF (1069K) -
MASARU KOBAYASHI, HIDEO FURUSE, HIROSHI MITSUHASHI1972 Volume 20 Issue 4 Pages 789-793
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReaction of sodium nitrite with enamine-type lactams (II and IX) was studied. The products were identified as oxime (III), ketone (IV and V), and nitrite (VI) from II and oxime (X), nitrimine (XI), and nitrite (XII) from IX. These were formed by initial attack of the nitroso ion on C-6 followed by concurrent fragmentation or hydrolysis. Formation of N-nitroso derivatives or deaza compounds was not observed.View full abstractDownload PDF (795K) -
TETSUYA NAKAMURA, SHIZUMASA KIJIMA1972 Volume 20 Issue 4 Pages 794-799
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThree phosphomethyl tocopheryl acetates: 7-phosphomethyl-β-tocopheryl acetate (IXa), 5-phosphomethyl-A-tocopheryl acetate (IXb), 5-phosphomethyl-δ-tocopheryl acetate (IXc), and their sodium salts (Xa), (Xb) have been synthesized starting from acetoxymethyl tocopheryl acetates by unequivocal way. These phosphates are of interest in a possible role of vitamin E in oxidative phosphorylation.View full abstractDownload PDF (935K) -
YOSHINARI HASEGAWA, TSUNEKI KANECHIKA, SUSUMU ISHIGURO, MASAO SEKIYA, ...1972 Volume 20 Issue 4 Pages 800-805
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSForty substituted phenyl glycosides and corresponding thioglycosides were synthesized and tested the tumor growth effect against sarcoma 180 with these compounds. Most of the aromatic thioglycosides markedly increased the tumor growth in weight. It seems that compound XIV or XVII possessed the highest activity among the compounds examined. One of most active substances accelerate a growth of the body weight in young mice and a regeneration of the partial hepatectomy in rats. On the other hand, these compounds have no immunosuppressive or activating effect.View full abstractDownload PDF (777K) -
TAISUKE MATSUO, TAKUICHI MIKI1972 Volume 20 Issue 4 Pages 806-814
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe Diels-Alder reaction of 4-carboxymethyl-5-ethoxyoxazole (I) was investigated. First, the mechanism and the stereochemistry of the adducts in the course of the Diels-Alder reaction were discussed. Second, the reaction of I with asymmetrical dienophiles gave the substance that an electron attracting group was preferentially introduced at γ-position of pyridine nucleus. Finally, the reaction of I with maleic anhydride, fumaric acid, maleic acid and methacrylic acid afforded the decarboxylated compounds. The mechanism of these reaction was discussed.View full abstractDownload PDF (1396K) -
MASAO SATO, MITSURU UCHIYAMA1972 Volume 20 Issue 4 Pages 815-822
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe effect of the long chain keto acid, which is one of the secondary products from oxidative deteriolation of lipids, on the enzyme activity was investigated in vitro. Cholinesterase and succinate dehydrogenase were inhibited more effectively by 12-keto oleic than by linoleic acid, whereas the inhibition of trypsin by linoleic acid was greater than that caused by 12-keto oleic acid. This fact may show that the enzyme inhibition 12-keto oleic acid is not merely due to nonspecific denaturation.
The inhibitory effect of 12-keto oleic acid on acetylcholinesterase was not protected the presence of a-tocopherol, while the inhibition by linoleic acid was completely restored when a-tocopherol was added simultaneously. When both linoleic and 12-keto oleic acids were added at the same time, the synergistic inhibition was observed, which partially protected by a-tocopherol. hus the inhibition caused by 12-keto oleic is not only the reflection of the stimulation of lipid peroxidation induced by 12-keto oleic acid, but the specific irreversible interaction with enzyme protein.View full abstractDownload PDF (1243K) -
YOSHIRO KOBAYASHI, ITSUMARO KUMADAKI, SHIGERU TAGUCHI1972 Volume 20 Issue 4 Pages 823-826
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReduction of (trifluoromethyl) quinolines by nucleophilic attack of hydride was studied. Sodium borohydride reduced only 3-(trifluoromethyl) quinoline to methyl derivative, while lithium aluminum hydride reduced other isomers to methylquinolines and 3-(trifluoromethyl) quinoline to 3-(difluoromethyl)-1, 2-dihydroquinoline. The mechanisms were proposed.View full abstractDownload PDF (626K) -
ZEN-ICHI HORII, SADAAKI FUJITA, YUTAKA OZAKI, MIYOJI HANAOKA, TAKEFUMI ...1972 Volume 20 Issue 4 Pages 827-829
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDownload PDF (521K) -
KOICHI MORI, YO UEDA1972 Volume 20 Issue 4 Pages 829-831
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSAlthough the physical properties of sulfonamide derivatives have been investigated in detai1, those of sulfinamide derivatives have been left almost in ambiguity. This paper deals with the results obtained from the infrared spectra of 25 aromatic sulfinamide derivatives measured in both CHCl3solution and KBr disks.View full abstractDownload PDF (506K) -
YOSHIFUMI MAKI, MIKIO SUZUKI1972 Volume 20 Issue 4 Pages 832-834
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDownload PDF (500K) -
IKUO MORIGUCHI, SHIZUO FUSHIMI, REIKO UMEHARA, NOBUYOSHI KANENIWA1972 Volume 20 Issue 4 Pages 834-836
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe molecular basis for the lowering action of chloroprmazine (CPZ) on the membrane permeability has not been cleared yet. The surface activity of CPZ itself has been thought to be ascribable to the permeability reduction for some time. However, Blei has demonstrated a marked decrease in the surface tension of solutions of CPZ in the presence of adenosine-5'-triphosphate (ATP), and suggested that the formation of CPZ-ATP complex of greater surface activity than CPZ alone is attributed to the reduction of membrane permeability. Hence, in the present work, the formation of complexes of CPZ with adenosine, adenosine-5'-monophosphate (AMP), and ATP has been investigated by the aid of ultraviolet absorption spectra.View full abstractDownload PDF (457K) -
TOYOSHIGE KABEYA, YOSUKE OHKURA1972 Volume 20 Issue 4 Pages 837-839
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIn a previous paper, a colorimetric method for the determination of urea nitrogen in blood and urine was presented on the basis of a color reaction of urea with diacetyl monoxime (DAM) in phosphoric acid solution in the presence of D-glucuronolactone (GL), which served to produce a photo-stable color and eliminate the sigmoidal nature of calibration curve observed usually in the DAM method. The method was then modified for the microdetermination and the automated determination of urea nitrogen in blood. These methods, however, required a relatively long heating time (40 min) to obtain an appropriate and constant intensity.
In the course of study on the determination of urea in biological fluids, D-gluco-1, 4-3, 6-disaccharolactone (SL) was found to produce rapidly an intense color when added to the reaction mixture of urea with DAM in phosphoric acid solution. The developed color gradually faded in daylight, but the initial color became stable when GL was present in the reaction mixture. Then a simple, rapid and reliable method for the determination of urea nitrogen in blood was developed utilizing this finding.View full abstractDownload PDF (448K) -
MITSUO SATO, TAKAO KWAN1972 Volume 20 Issue 4 Pages 840-841
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSPetroleum crudes contain metal porphyrins which are known to poison catalysts when the petroleum is subjected to a catalytic hydrodesulfurization. During the course of our hydrodesulfurization studies, some preliminary investigations on the chromatographic separation of metal porphyrins were carried out, leading us to consider that a thin-layer chromatographic separation is superior and less time-consuming as compared with the paper chromatographic method. In the present note we shall report such a thin-layer chromatographic method with respect to the separation of synthetic tetraphenylporphin and its metal complexes.View full abstractDownload PDF (307K) -
TOSHIO NAMBARA, YASUHIKO MATSUKI, NORIKO MIYAZAKI1972 Volume 20 Issue 4 Pages 842-845
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
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MICHIO MATSUI, FUKUO ABE, YASUYO WATANABE, TAMAE WANIBE, MASASHI OKADA1972 Volume 20 Issue 4 Pages 845-848
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIn connection with the biochemical studies on D-glucaric acid, a normal constituent of human urine which is derived from D-glucuronolactone, we developed a colorimetric method for the quantitative determination of this acid. Thus, D-glucaric acid separated from mammalian urines using ion-exchange column chromatography was oxidized with periodic acid to give glyoxylic acid, which was further converted into the intensely colored 1, 5-diphenyl-formazan and determined colorimetrically. During the course of our studies on D-glucaric acid a much more highly sensitive method was required for the accurate estimation of normal serum level of D-glucaric acid in mammals. The present paper deals with the fluorometric determination of D-glucaric acid which is based on the condensation of glyoxylic acid derived from D-glucaric acid with 4'-hydrazino-2-stilbazole to yield a highly fluorescent product using a modification of the procedure for the determination of α-oxo acids originally reported by Mizutani, et al.(Fig. 1).View full abstractDownload PDF (557K) -
HARUO OGURA, MASARU OGIWARA1972 Volume 20 Issue 4 Pages 848-850
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
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HIROSHI HIKINO, YASUSHI OHIZUMI, TOMOKO SAITO, ETSUKO NAKAMURA, TSUNEM ...1972 Volume 20 Issue 4 Pages 851-853
Published: April 25, 1972
Released on J-STAGE: January 31, 2011
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TOSHIO NAMBARA, TAKAKO ANJYO, HIROSHI HOSODA1972 Volume 20 Issue 4 Pages 853-854
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
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ISAMU MURAKOSHI, HIROYUKI KURAMOTO, SHIGERU OHMIYA, JOJU HAGINIWA1972 Volume 20 Issue 4 Pages 855-857
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
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JUNJI NAKANO, HITOSHI UNO1972 Volume 20 Issue 4 Pages 857-859
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
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HISASHI ISHII, KATSUHIRO HOSOYA1972 Volume 20 Issue 4 Pages 860
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDownload PDF (159K) -
JINSAKU SAKAKIBARA, KATSUSHIGE IKAI, MASAITI YASUE1972 Volume 20 Issue 4 Pages 861-862
Published: April 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDownload PDF (232K)
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