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Volume 17, Issue 7
Displaying 1-36 of 36 articles from this issue
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ISOO ITO, TAISEI UEDA1969 Volume 17 Issue 7 Pages 1309-1315
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFor pharmacological evaluation of new improved antipyretic and analgesic agents, several kinds of 3-mercaptomethyl-2-methyl-1-phenyl-3-pyrazolin-5-one derivatives were synthesized. The reaction between 2, 4-dimethyl-3-mercaptomethyl-1-phenyl-3-pyrazolin-5-one (I) and 2-nitrochlorobenzene (XVIII) in the presence of sodium ethoxide under colling with ice gave bis (2, 4-dimethyl-5-oxo-1-phenyl-3-pyrazolin-3-yl)-trans-ethylene (XXIV) and 2-nitrobenzenethiol (XXVII) in addition to the objective compound (XXI). The same reaction under reflux afforded 2, 4-dimethyl-5-oxo-1-phenyl-3-pyrazolin-3-carboxylic acid (XXX) and bis (2-nitrophenyl) sulfide (XXXII) as by-products. These by-products were proved to be formed by the splitting of XXI in the presence of sodium ethoxide. The improved synthesis was effected by using dimethylformamide as an aprotic solvent without the formation of undesirable substances.View full abstractDownload PDF (779K) -
KINZO NAGASAWA, HISAE YOSHIDOME1969 Volume 17 Issue 7 Pages 1316-1323
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn a solution containing the polar solvent such as pyridine, quinoline, dioxane, dimethylformamide, and dimethylsulfoxide, sulfamic acid and its N-substituted derivatives were converted to an equimolar amount of inorganic sulfate and corresponding amine. The factors and the reaction mechanisms concerning this degradation process were discussed on the basis of the experimental results, and the following scheme of the reaction was proposed : [chemical formula] It was also proved that this reaction and the determination procedures is possible to apply as the general analytical method for sulfamic acid derivatives.View full abstractDownload PDF (872K) -
KATSUYA ENDO, PAULDE MAYO1969 Volume 17 Issue 7 Pages 1324-1331
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of α-vetivone, one of the major odoriferous principles of vetiver oil had previously been accepted as being represented by Ia. Air oxidation of α-vetivone in the presence of 1N t-butoxide yielded, after treatment with p-toluenesulphonic acid, a conjugated dienedione VII. The enantiomeric compound was prepared, by oxidation, from the structurally well-established eremophilone XII, thus requiring that the structure of α-vetivone be revised to II. Some interesting observations were made with regards ORD and CD measurements in comparison with curves obtained from cholest-4-en-3-one. Biogenetic relationships between some related compounds are also discussed.View full abstractDownload PDF (897K) -
KIICHIRO KAKEMI, HITOSHI SEZAKI, KATSUHIKO OKUMURA, SHINICHIRO ASHIDA1969 Volume 17 Issue 7 Pages 1332-1338
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAqueous solutions of seven isonicotinic acid derivatives were injected to the hind leg of rats and the intramuscular absorption was followed by the local clearance method for a period of 5 min under the conditions in which the constant body temperature and smaller injection volume were maintained. Drug absorption is proportional to the amount remaining in the injection site, and both molecular weight and partition coefficient of drugs affect the intramuscular absorption. The observation presented here supported the conclusion that (1) the abscrption of unionized drugs from the injection site was chiefly proceeded by the apparent first order process and (2) the diffusion through the pores of the capillary vessels was predominant compared with the penetration through the capillary endothelial cells. In the case of ionized drugs, there was evidence that the absorption of a drug was influenced by the factor other than the above.View full abstractDownload PDF (820K) -
Spectroscopic Studies on Molecular Interactions. I. Complexations between Caffeine and Benzoic AcidsIKUO MORIGUCHI, MIHOKO NAYUKI, NOBUYOSHI KANENIWA1969 Volume 17 Issue 7 Pages 1339-1343
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSInteractions between caffeine and 21 un-and mono-substituted benzoic acids were investigated at pH 7.0 and 30°by means of an indirect method utilizing the spectral change due to the competition between congo red and benzoates in complexation with caffeine. The main molar composition of the complexes appeared to be 1 : 1, and apparent equilibrium constant and free energy change for the complex formation were evaluated. The relation between the free energy change and pKa for benzoates suggested that direct electrostatic forces between the carboxyl group in the benzoate molecules and the nitrogen of the 7-position in the caffeine molecule played a dominant role in the complexations.View full abstractDownload PDF (546K) -
MISAKO ARAKI, YUTAKA KAWAZOE, CHIKAYOSHI NAGATA1969 Volume 17 Issue 7 Pages 1344-1351
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSO, O'-Diacetyl-4-hydroxyaminoquinoline 1-oxide was found easily to liberate a considerable amount of acetic acid in inert organic solvents such as dioxane as well as in crystalline form. The acetic acid formation was regarded as being initiated by homolytic fission of N-O bond of the substituent hydroxyamino group and studied with a help of electron spin resonance spectroscopy. A brief discussion was made of the correlation of free radical formation with carcinogenesis of carcinogenic hydroxylamine derivatives.View full abstractDownload PDF (824K) -
TADAHIKO OTAKA, MITSURU UCHIYAMA, TSUNEMATSU TAKEMOTO, HIROSHI HIKINO1969 Volume 17 Issue 7 Pages 1352-1355
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe insect-metamorphosing steroids obtained from ferns were assayed in terms of their ability to stimulate protein synthesis in mouse liver. Ponasterone A, pterosterone. ecdysterone, shidasterone and lemmasterone possessing hydroxyls at C-20 and C-22, showed high activity. However, polypodine B (5β-hydroxyecdysterone) was much less active in acceleration. Ponasteroside A (ponasterone A 3-β-D-glucopyranoside) also revealed anabolic potency. On the other hand, ecdysone, having a hydroxyl at C-22 but not at C-20, exhibited little stimulation.View full abstractDownload PDF (437K) -
AKIRA TAKAMIZAWA, YOSHIO HAMASHIMA, HISAO SATO, SHOJI SAKAI1969 Volume 17 Issue 7 Pages 1356-1362
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactions of diethyl acetyl-and diethyl benzoylphosphonate (2, 3) with 3, 4-dimethylthiazolium bromide (8) afforded 2-(1-diethylphosphoroyl) ethyl-and 2-(1-diethyl-phosphoroyl) benzyl-3, 4-dimethylthiazolium bromides (9, 10), which were decomposed to give 2-methyl-and 2-phenyl-4, 5-dimethyl-2, 3-dihydro-4H-1, 4-thiazin-3-ones (11, 12) by alkaline treatment. The reactions of 8 with dimethyl acetyl-and dimethyl benzoyl-phosphonate (13, 14) gave the inner salts of O-methyl-O-1-(3, 4-dimethyl-2-thiazolium)-ethyl-and O-methyl-O-1-(3, 4-dimethyl-2-thiazolium) benzyl phosphoric acid (15, 16). Similar adducts (18, 24) were obtained from the reactions of 1b with 13 and 14. In a careful treatment, the inner salt (26) was found to be produced from 2-(1-diethylphos-phoroyl) ethyl-3-benzyl-4-methyl-5-(2-benzoyloxy) ethylthiazolium bromide (4).View full abstractDownload PDF (826K) -
YOSHIO ARATA, SHIGEYUKI YOSHIFUJI, YOSHIHIRO YASUDA1969 Volume 17 Issue 7 Pages 1363-1368
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS10-Cyano-5-methyloctahydroquinolizinium iodide (V) was treated with silver oxide to give carbamoyl methohydroxide (VI), which was further converted to carbamoyl methobromide (VII). Reaction of V and VII with lithium in liquid ammonia afforded 1-methylazecane (IX) and 10-cyano-1-methylazecane (VIII), and 1-methylazecane-6-carboxamide (XI) and a demethylated compound (IX), respectively. 10-Amino-5-methyloctahydroquinolizinium bromide (XIV) which was derived from VII was heated in an alkaline solution affording 1-methyl-6-azecanone (XV), whose ring appears in the majority of the medium sized ring alkaloids.View full abstractDownload PDF (764K) -
KAZUMOTO MIYAHARA, TOSHIO KAWASAKI1969 Volume 17 Issue 7 Pages 1369-1376
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPure tokoronin, mp 275-277°(decomp.), [α]D-13.2°, was obtained in an improved method from the ethanol extracts of rhizomes of Dioscorea tokoro MAKINO and the structure was established as tokorogenin (25D, 5β-spirostane-1β, 2β, 3α-triol)-1-O-α-L-arabinopyranoside (XVII). It represents an additional example of a novel type of spirostanol glycoside in which the sugar moiety is combined with a hydroxyl group other than that at C-3 of the aglycone.View full abstractDownload PDF (909K) -
ISAO SUGIMOTO1969 Volume 17 Issue 7 Pages 1377-1382
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffect of complex formation on the drug absorption from the rat small intestine by the perfusion method in situ was investigated. Apparent absorption rate of carbazochrome or nicotinamide alone was compared with that together its complexing drug. As the complexing drugs of carbazochrome, the following drugs were used : nicotinamide, 7-(2-hydroxyethyl) theophylline (HET), caffeine, 7-(2, 3-dihydroxypropyl) theophylline sodium (DHPT), and p-aminosalicylate (NaPAS). HET was used as the complexing drug of nicotinamide. It was found that the apparent absorption rate of carbazochrome was enhanced by complex formation with HET and caffeine at pH 3.0 and 4.7, and with NaPAS at pH 6.0, and that there was no significant difference in the apparent absorption rate between alone and together the complexing drug in nicotinamide-HET at pH 3.0 and 3.9, in carbazochrome-nicotinamide at pH3.0 and 3.9, and in carbazochrome-DHPT at pH6.0. From these absorption experiments and physico-chemical property for the complex, it is assumed that an extent of molecular interaction and the difference between the absorption rate of the drug and that of its complexing drug affect the absorption of the complex.View full abstractDownload PDF (706K) -
ISAO MATSUNAGA, ZENZO TAMURA1969 Volume 17 Issue 7 Pages 1383-1389
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was found that a lactone ring was esterified to a methyl ester group in the bufferized methanol containing triethylamine-acetic acid or sodium acetate without simultaneous cleavage of the acyl groups and the methyl ester groups and this methanolysis mainly proceeded without acyl migration. Using this method, 2, 4-O-benzylidene-5-O-acyl-D-glucaro-6, 3-lactone 1-methyl esters (II, III, IV and V) were esterified in excellent yields to dimethyl 2, 4-O-benzylidene-5-O-acyl-D-glucarates (VII, VIII, IX and X respectively), and from the latters, dimethyl 2, 4-O-benzylidene-3-O-acetyl-5-O-acyl-D-glucarates (XI, XII, XIII and XIV respectively) were synthesized by the usual acetylation. Moreover, 1, 2-O-isopropylidene-5-O-acetyl-D-glucofuranurono-6, 3-lactone (XIX) could be also esterified to methyl 1, 2-O-isopropylidene-5-O-acetyl-D-glucofuranuronate (XX) by the same method.View full abstractDownload PDF (788K) -
HIROSHI HIKINO, KEITARO AOTA, TSUNEMATSU TAKEMOTO1969 Volume 17 Issue 7 Pages 1390-1394
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo norsesquiterpenoids, kobusone and isokobusone, have been newly isolated from nutgrass, Cyperus rotundus (Cyperaceae), and shown to have the stereostructures I and VII, respectively, by the spectral properties of them and their derivatives and by transformation of caryophyllene oxide (VI) to the oxido-ketone (I) which has further been converted into the keto-alcohol (VII).View full abstractDownload PDF (692K) -
DAISUKE SATOH, MIEKO MIYAMURA, SETSUKO NISHII1969 Volume 17 Issue 7 Pages 1395-1400
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the results of lead tetraacetate oxidation of γ-digiprogenin 3-acetate as well as sodium metaperiodate oxidation of tetrahydro-γ-digiprogenin 3-acetate, the position of the tertiary hydroxyl group was revised to C-14 from C-17, and the new structure, 3β, 14-dihydroxy-14β, 17β-pregn-5-ene-11, 15, 20-trione (VIIIa) was assigned to γ-digiprogenin. α-Digiprogenin is its 17-epimer (IXa).View full abstractDownload PDF (694K) -
DAISUKE SATOH, SETSUKO NISHII1969 Volume 17 Issue 7 Pages 1401-1404
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS14-Position of the tertiary hydroxyl group of γ-and α-digiprogenin (I and II) was established by partial synthesis of dihydro-α-digiprogenin 3-acetate (IIIb) from 11-oxo-tigogenin 3-acetate. Dehydration mechanism of α-digiprogenin (14-hydroxy-15, 20-dione type) to β-digiprogenin (16-ene-15, 20-dione type) was presented.View full abstractDownload PDF (612K) -
SADAO OIDA, EIJI OHKI1969 Volume 17 Issue 7 Pages 1405-1421
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEpoxidation of 2-(p-methoxyphenylmethyl)-1-benzyloxycarbonyl-3-pyrroline (39) with pertrifluoroacetic acid gave 3α, 4α-epoxide (40) and 3β, 4β-epoxide (41). Acetolysis of 41 predominantly yielded 4α-acetoxy-3β-hydroxypyrrolidine (43), which was converted into the α-epoxide (40) by mesylation and successive treatment with bases. Treatment of the α-epoxide (40) with trifluoroacetic acid, followed by acetylation and removal of the protecting groups gave 4α-acetoxy-3β-hydroxypyrrolidine (47) and dl-anisomycin (1). 1 showed superimposed infrared and nuclear magnetic resonance spectra with those of natural anisomycin and exhibited one-half the activity against Candida albicans. In addition, the epoxide-cleavage reaction of these 3, 4-epoxypyrrolidines was discussed.View full abstractDownload PDF (2051K) -
TOKUJI SUZUKI, YUICHI TANIMURA1969 Volume 17 Issue 7 Pages 1422-1431
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe quantitative procedure of nicotinic acid liberated from meso-inositol hexanicotinate (IHN) and several nicotinic acid esters of polyhydric alcohols and the stability in acidic solution were investigated to predict the gastric stability for a possible explanation of their absorption from the gastrointestinal tract. Nicotinic acid formed by the degradation could be satisfactorily separated from the other degraded products by the ion-exchange chromatography. The results were in agreement with those of the titrimetry. The thinlayer chromatography on the degradation of IHN showed that IHN was solvolyzed to many intermediates which then successively decomposed to further degraded products. The initial solvolytic rate of IHN in 0.1N HCl and at 37.0°was faster than about ten times those of the other nicotinic acid esters used. The observed rate of the degradation of IHN was first order with respect to IHN concentration at a constant temperature and hydrogen ion concentrations by the thin-layer chromatographic technique. The variation of the rate constant was minor in the range of 0.04 to 1.0N HCl and at 37.0°. The dissolution of IHN from tablets, the enzymatic stability and the solubility of IHN were also discussed.View full abstractDownload PDF (1139K) -
SHOJI OKADA, OSAMU TAMEMASA1969 Volume 17 Issue 7 Pages 1432-1437
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAntibiological actions were studied on 2-amino-1, 4-naphthoquinone imine-HCl (ANQI), which had been investigated in vitro as a potent inhibitor of DNA synthesis in Ehrlich mouse ascites tumor cells and as an interacting substance to DNA. The results are as follows : 1. Antimicrobial Action : A considerable activity was found against animal and plant microorganisms, especially Xanthomonas oryzae. 2. Acute Mammalian Toxicity : LD50 was 5.45 (4.88-6.09) mg/kg in mice (intraperitoneal injection). Only a little and transient effect was observed on behaviors of mice, and on respiration and blood pressure of dogs. 3. Antitumor Activity : ANQI exerted no therapeutic effect on Ehrlich mouse ascites tumor in vivo, but shortened survival days of tumor-bearing mice in its high doses. 4. Chemical Changes in Mouse Ascitic Fluid : ANQI in part was oxidized in ascitic fluid of tumor-bearing mice to 2-amino-1, 4-naphthoquinone, which had been found to be not inhibitory to nucleic acid synthesis. The ineffectiveness of ANQI on the tumor in vivo was parlty explained from the susceptibility to biological oxidation.View full abstractDownload PDF (677K) -
MASAHIRO NAGAI, KAZUO IZAWA, TAKAO INOUE1969 Volume 17 Issue 7 Pages 1438-1443
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the rhizoma of Peltoboykinia tellimoides (MAXIM.) HARA, two triterpene acids were isolated. One of them, a new triterpene, named β-peltoboykinolic acid (I), mp 220-222°(decomp.), [α]24D+114°, has been established to be olean-12-ene-3β-ol-27-oic acid and another, named α-peltoboykinolic acid (II), mp 234-236°, [α]17D+121°, to be urs-12-ene-3β-ol-27-oic acid, which is identical with a compound derived from quinovic acid by L. Ruzicka, et al. in 1946. These are the first examples of naturally occurring triterpene acids with the only carboxyl group at C-27 of ursane and oleanane types.View full abstractDownload PDF (751K) -
MASARU AOKI, AKIRA KAMADA, HIROSHI FUKUCHI, YASUKO SUMIYAMA1969 Volume 17 Issue 7 Pages 1444-1449
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSedimentation and flocculation of dispersed phase were studied using Newtonian and non-Newtonian suspensions of calcium carbonate. The constant K in the Robinson equation proved to be dependent upon the degree of flocculation rather than upon particle shape and roughness only as was previously reported by Robinson. It was also revealed that the K was closely related to the structural viscosity of suspension, showing a figure near to 4 for Newtonian suspension and larger than 4 as the suspension's structural viscosity increased. Relations were also studied between the volume of the immobilized medium on particle surface and the structural viscosity of suspension. It was revealed that the volume of the immobilized medium on particle surface varied depending upon the kind of suspending medium and the larger the volume of the immobilized medium the greater the relative effect on structural viscosity.View full abstractDownload PDF (729K) -
HISASHI NOGAMI, TSUNEJI NAGAI, EIHEI FUKUOKA, TAKASHI SONOBE1969 Volume 17 Issue 7 Pages 1450-1455
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAspirin (ASP) tablet containing potato starch (PS) (ASP+PS) generally took a short disintegration time. ASP tablet containing microcrystalline cellulose (MCC) (ASP+MCC) showed an optimum concentration region of MCC to give a minimum disintegration time, while (ASP+PS) did not. From the data of water intake and swelling of the powder beds of PS and MCC, PS was more affinitive to water than MCC, and from the data of capillarity, hardness and disintegration of (ASP+PS) and (ASP+MCC), it was concluded that both the mean capillary diameter and the hardness were not always correlated with the disintegration time. Taking these results into consideration, the mechanism of tablet disintegration was. discussed on the basis of cohesive and adhesive properties of particles. Finally, it might be concluded that the penetration of water into a tablet was necessary for the disintegration as the first step without being sufficient and that the work of dispersion of particles caused through the penetration of water had to overcome the binding work of particles caused through cohesion and adhesion, accordingly giving an optimum mixing ratio of drug and additive, as was shown by (ASP+MCC).View full abstractDownload PDF (763K) -
DAISUKE SATOH, JUNKO MORITA1969 Volume 17 Issue 7 Pages 1456-1461
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe order of acetylation of four hydroxyl groups in the sugar moieties of digitoxin (Ia) was revised to be 4'''→3'''→3''-or 3'-positions by the results of acetyl migration test and cis-glycol test as well as modified controlled polysaccharide degradation method using metaperiodate. Nuclear magnetic resonance (NMR) spectra of several acetates of Ia were examined, and the conformations of digitoxose moieties of Ia were confirmed to be all C1-form as formula XIa from the NMR data and reactiviteis of hydroxyl groups in acetylation.View full abstractDownload PDF (766K) -
AKIRA TAKAMIZAWA, KENTARO HIRAI, YOSHIO HAMASHIMA, HISAO SATO1969 Volume 17 Issue 7 Pages 1462-1466
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-Methylbenzoxazolium, N-methylbenzothiazolium, and benzimidazolium salts were reacted with triethylamine, potassium t-butoxide or dimsyl sodium to give corresponding ketospiran derivatives. Several other products were also characterized and possible mechanisms of these reactions were discussed briefly.View full abstractDownload PDF (632K) -
TAKEO NAITO, TORU YOSHIKAWA, SHINICHI KITAHARA, NAOEMON AOKI1969 Volume 17 Issue 7 Pages 1467-1478
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to find new analgesics and anti-inflammatories, 1-and 2-pyrimidinyl-3-methylpyrazolin-5-one derivatives (III and VII) were synthesized from hydrazinopyrimidines (I) and ethyl acetoacetate or ketene dimer, and then methylated to afford 1-and 2-pyrimidinyl-3-methyl-5-methoxypyrazoles (IV and VIII), 1-pyrimidinyl-2, 3-dimethylpyrazolin-5-ones (V), and 2-pyrimidinyl-1, 3-dimethylpyrazolin-5-ones (IX). Physical properties of these derivatives were also described.View full abstractDownload PDF (984K) -
RENZO DOHMORI, YOSHIAKI NAKAI, RYUICHI YOSHIMURA, TAKEO NAITO1969 Volume 17 Issue 7 Pages 1479-1484
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe ring closure of N2-pyrimidinyl-3-oxobutyrohydrazide derivatives by fusion was studied and a novel method for the synthesis of 1-pyrimidinyl-3-methylpyrazolin-5-one derivatives was found. This reaction mechanism was also investigated and a hypothesis was presented for the reaction process which includes an intermolecular rearrangement.View full abstractDownload PDF (765K) -
MITSUJI SANO, ISAO ITOH, YOSHIAKI NAKAI, TAKEO NAITO1969 Volume 17 Issue 7 Pages 1485-1491
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe tautomerism of 1-and 2-pyrimidinylpyrazolin-5-ones was investigated by using the combination of spectral methods, IR, NMR, and UV. 1-Pyrimidinylpyrazolin-5-ones exist in NH and OH forms in nonpolar media such as chloroform and carbon tetrachloride, while NH form increases in aqueous solution. In nonpolar media 2-pyrimidinylpyrazolin-5-ones exist predominantly in the OH form, although in aqueous solution, they are mostly in NH form.View full abstractDownload PDF (712K) -
YASUO OSHIMA, TAKESHI AKIMOTO, WATARU TSUKADA, TERUKIYO YAMASAKI, KUNI ...1969 Volume 17 Issue 7 Pages 1492-1497
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to search for a highly potent drug, 1-and 2-pyrimidinylpyrazole derivatives have been examined for analgesic, antipyretic and anti-inflammatory activities. Among the 44 derivatives examined in this series, all of the compounds which are equal to or more potent than aminopyrine in analgesic activity were found to belong to 1-pyrimidinylpyrazole type, while all of 2-pyrimidinylpyrazole derivatives were extremely less active than aminopyrine in analgesic effect. Three compounds which possess a methoxyl group in the 5-position of the pyrazole moiety were found to have especially high potency in this series. It has been found that 1-(4-methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole is the most potent compound having analgesic and anti-inflammatory effects.View full abstractDownload PDF (591K) -
AKIRA MINATO, SEIYU HIROSE, TAKETO OGISO, KEIKO UDA, YUKIO TAKIGAWA, E ...1969 Volume 17 Issue 7 Pages 1498-1504
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1) Taurine-35S was injected intravenously to rats and the radioactivity in tissues, bile, urine and feces was measured at various time intervals after the administration. 2) Taurine-35S was rapidly eliminated from the blood stream almost regardless of its dosage levels examined. The largest accumulation of radioactivity in the earlier periods was found in the kidney, liver and small intestine. The spleen and lung followed them. The least uptake of 35S was observed with the brain. 3) The radioactivity in the heart, diaphragm and muscle increased gradually, whereas that in the other organs decreased. 4) As for the intracellular localization, radioactivity was present in the soluble fraction of all the tissue homogenates tested. 5) 35S readily appeared in the bile, wherein free taurine-35S as well as its conjugates with bile acids was recognized. 6) A large, initial uptake of 35S by the intestinal walls was found to be essentially independent of the reabsorption of radioactive biliary components. 7) No particular accumulation of taurine-35S was noticed in a newly formed granuloma tissue within the limits of the present study.View full abstractDownload PDF (836K) -
AKIO TSUJI, TOSHIO KINOSHITA, MASANORI HOSHINO1969 Volume 17 Issue 7 Pages 1505-1510
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel method for determination of hexosamines was established utilizing 3-methyl-2-benzothiazolone hydrazone hydrochloride (MBTH) and ferric chloride. This method was highly sensitive and specific. All the procedure was carried out in mildly acidic aqueous solution at room temperature. The hexosamine content of chondroitin sulfates and hyaluronic acid estimated by this method showed good agreement with that calculated from nitrogen contents of the polysaccharides. Moreover, only 2 hr of hydrolysis with 2N hydrochloric acid was sufficient for the assay of these mucopolysaccharides.View full abstractDownload PDF (685K) -
YOSHIRO KOBAYASHI, ITSUMARO KUMADAKI, KUNIO MORINAGA1969 Volume 17 Issue 7 Pages 1511-1514
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1, 6-Phenanthroline was synthesized from 4-aminoquinoline by the Skraup reaction using sulfo-mix, and N-oxidation was carried out in various ways to obtain 6-oxide and 1, 6-dioxide. Reactions of 6-oxide with acetic anhydride and with phosphoryl chloride and the Reissert reaction were carreid out and the results were compared with those in the case of 1, 6-naphthyridine.View full abstractDownload PDF (622K) -
YOSHIO SASAKI, MIYOKO SUZUKI, MASAO HATTORI1969 Volume 17 Issue 7 Pages 1515-1517
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (390K) -
MASAICHIRO MASUI, CHINO YIJIMA1969 Volume 17 Issue 7 Pages 1517-1521
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
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KUNIO NAKAGAWA, HIROSHI ONOUE, KYOJI MINAMI1969 Volume 17 Issue 7 Pages 1522-1523
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (368K) -
ISOO ITO, NORIICHI ODA, KATSUHIKO TAKEDA, TAKAHIRO WAKAYAMA1969 Volume 17 Issue 7 Pages 1524-1526
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (472K) -
AKIRA TAHARA, YASUO OHTSUKA1969 Volume 17 Issue 7 Pages 1529-1531
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
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TOSHIO MIYAZAKI, J.K.N. JONES1969 Volume 17 Issue 7 Pages 1531-1533
Published: July 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (418K)
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