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Volume 25, Issue 4
Displaying 1-49 of 49 articles from this issue
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TAKEO HIGASHINO, YOSHIHISA IWAI, EISAKU HAYASHI1977 Volume 25 Issue 4 Pages 535-542
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe direct reaction of 1, 5-dimethyl-(XIm), 5-methyl-1-phenyl-1H-pyrazolo [3, 4-d]-pyrimidinium iodide (XIp), 1-methyl-(XIIm), and 1-phenyl-1H-pyrazolo [3, 4-d] pyrimidinium hydrogen sulfate (XIIp) with active methylene compound and ketone (NuH) were carried out. NuH used in this study were as follows : malononitrile (NuH-1), ethyl cyanoacetate (NuH-2), ethyl acetoacetate (NuH-3), ethyl benzoylacetate (NuH-4), acetylacetone (NuH-5), acetone (NuH-6), cyclopentanone (NuH-7), cyclohexanone (NuH-8), and acetophenone (NuH-9). Thus, XI was transformed into the 5, 6-disubstituted 1-methyl-(or 1-phenyl)-1H-pyrazolo [3, 4-b] pyridines (IX) by the direct reaction with NuH in butanol. Similar transformation took place in the reaction of XII with NuH yielding IX together with 5-amino-1-methyl (or 1-phenyl)-1H-pyrazole (XIV). These 1H-pyrazolo [3, 4-b] pyridines (IX) were also prepared by the Friedlaender synthesis with 5-amino-1-methyl (or phenyl)-1H-pyrazole-4-carboxaldehyde (XV) and NuH in the presence of ethoxide ion. The three possible reaction mechanisms ; path A, B, and C, were proposed. And it might be concluded that the path A stood to reason than the path B or C for the ring transformation of XI and it was not clear which path of A, B or C, was the most suitable for the ring transformation of XII.View full abstractDownload PDF (873K) -
TOYOZO TAKADA, YOSHIYUKI KOSUGI, MITSUO AKIBA1977 Volume 25 Issue 4 Pages 543-547
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermolysis of 2-acetyl-3, 6-diamino-5-methyl-1, 4-benzoquinone tosylhydrazones (2a-c) prepared by the reactions of monoaminoquinone tosylhydrazones (1a-c) with the corresponding amines gave 5-hydroxyindoloquinones (5a, b) and related compounds. In the case of 2-acetyl-5-methyl-6-morpholino-3-pyrrolidino-1, 4-benzoquinone tosylhydrazone (2e), 7-morpholino-(4e) and 7-hydroxypyrrolo [1, 2-α] indoloquinone (5a) were obtained. The mechanism of this reaction, which afforded new indoloquinone ring systems, was investigated.View full abstractDownload PDF (655K) -
FARONKH. AL-HAJJAR, MOHAMEDS. EL-EZABY, NIZARR. EL-RAYYES1977 Volume 25 Issue 4 Pages 548-555
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAroylphenylacetylenes (I) reacted with N, N-dimethylhydrazine (II) to give 1, 1-dimethyl-2-[β-(α-aroylstyryl)] hydrazine (III). The structure and configuration of the products are based on chemical and spectroscopic evidence. The protonation constants of these compounds were calculated in 60 wt % dimethylformamide-water media. The effects of substituents on the protonation equilibria are discussed. The log β values were linearly correlated with Hammett substituent constant. The equation of the straight line : log β=(-0.52±0.049)σ+(3.86±0.02).View full abstractDownload PDF (747K) -
HIROMI TERAUCHI, KEIKO KOWATA, TOSHIE MINEMATSU, SHOJI TAKEMURA1977 Volume 25 Issue 4 Pages 556-562
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN, N-Dibromourethan (DBU) was prepared. The addition of DBU to styrene gave an anti-Markownikoff's adduct, (2). The orientation of the addition of DBU is thus similar to that of N, N-dichloro analogue (DCU) and opposed to that of N, N-dibromobenzenesulfonamide (DBBS). Reactions of DBU, DCU, and DBBS or N, N-dibromo-p-toluenesulfonamide with 1, 2-dihydronaphthalene were examined in which DBBS gave desired adduct, (5), in good yield whereas DCU and DBU gave no normal adduct but complex mixtures. Reaction of methyldihydronaphthalenes with these reagents gave similar results. Compound (2) was converted to 1-bromo-2-benzenesulfonamido (7), and 1-alkoxy-2-benzenesulfonamido-1, 2, 3, 4-tetrahydronaphthalenes (8 and 9).View full abstractDownload PDF (732K) -
SHIGEO SENDA, MIKIO SUZUKI, MIKIO TAKAHASHI, KOSAKU HIROTA1977 Volume 25 Issue 4 Pages 563-568
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIrradiation of 1, 3-dimethyl-5-nitro-6-styryluracils (1a-c) principally gave 1, 3-dimethyl-6-phenylpyrrolo [3, 2-d] pyrimidines (3a-c) in 8-16% yields. Irradiation of 6-anilino-5-nitrouracils (5a-c) gave alloxazines (6a, b) and isoalloxazine (6c) in 14-18% yields. These products were formed by photoreductive cyclization of a nitro group with an o-substituted styryl or anilino group.View full abstractDownload PDF (563K) -
HIROSHI KOBAYASHI, TSOCHIN PENG, RURIKO KAWAMURA, SHOZO MURANISHI, HIT ...1977 Volume 25 Issue 4 Pages 569-574
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe mechanism of absorption inhibitory effect of polysorbate 80 was investigated. The following observations were demonstrated. 1) No significant difference in the uptake of drugs by the muscles either in the presence or absence of polysorbate 80 could be demonstrated. 2) Succinylcholine chloride was used as a muscle relaxant, but no detectable difference in the absorption of isonicotinamide in the presence or absence of polysorbate 80 could be observed. Therefore the effect of polysorbate 80 on the contractility of the muscles was excluded. 3) There was a marked inhibition in the distribution rate of isonicotinamide from blood to muscle, and the extracellular spaces were greatly decreased by pretreatment with polysorbate 80. 4) Permeation of drug through muscle slices and the connective tissue permeability were significantly lowered in the presence of polysorbate 80. Therefore it can be concluded that the mechanism of the absorption inhibitory effect of polysorbate 80 was mainly due to its influence on the extracellular space and the connective tissue permeability.View full abstractDownload PDF (686K) -
MORIO IKEHARA, YUKO OGISO, TOKUMI MARUYAMA1977 Volume 25 Issue 4 Pages 575-578
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdenosine was allowed to react with t-butyl hypochlorite in a variety of conditions. Using limited amount of the chlorinating agent at low temperature (-70°) a monochloro compound (IIa) was obtained. The structure of IIa was tentatively assigned as N6-chloroadenosine. When the chlorination was conducted at higher temperature using excess reagent in dimethylformamide (DMF), 8-chloroadenosine (IIIa) was obtained as the main product. The structure of IIIa was elucidated by ultraviolet, mass and nuclear magnetic resonance spectra together with their chemical reactivities. The chlorination of 2', 3', 5'-tri-O-acetyladenosine also afforded 8-chloro derivative (IIIb) which gave 8-chloroadenosine by the treatment with ammonia. When N6-methyl or N6-dimethyladenosine were chlorinated using t-butyl hypochlorite only in the former case N6-chloro compound (IIc) was obtained. 8-Chloro-N6-methyl and-N6-dimethyladenosine (IIIc, d) were obtained when the chlorination was conducted in DMF as the solvent using excess t-butyl hypochlorite.View full abstractDownload PDF (644K) -
EISAKU HAYASHI, MITSUHISA IINUMA, IWAO UTSUNOMIYA, CHIHOKO IIJIMA, ETS ...1977 Volume 25 Issue 4 Pages 579-589
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe Grignard reactions of 1-phthalazine-(V-0), 2-quinoxaline (VI-0), and 4-cinnolinecarbonitrile (VII-0) were carried out. Grignard reagent used in this study was as follows ; phenylmagnesium bromide, benzylmagnesium chloride, isopropylmagnesium bromide, ethylmagnesium bromide, and methylmagnesium iodide. When a mixture of V-0 and Grignard reagent in tetrahydrofuran (THF) was refluxed for 3 hr, 1-alkylphthalazine (Va), 4-alkyl-3, 4-dihydro-1-phthalazinecarbonitrile (Vc), 4-alkyl-1-phthalazinecarbonitrile (Vc'), 2-alkyl-1(2H)-phthalazinone (Vd), and 4-alkyl-3, 4-dihydro-3-(1-phthalazinyl)-1-phthalazinecarbonitrile (Ve) were formed together with 1-benzoylphthalazine (Vb-1), 1, 4-diethyl-phthalazine (Vf-4), 1, 2-dihydro-1, 1, 2-triethyl-phthalazine (Vg-4), and 3, 4-dimethyl-3, 4-dihydro-1-phthalazinecarbonitrile (Vh-5), although the yields of all products were small. The reaction of VI-0 in THF carried out under the same conditions as V-0 gave 2-alkylquinoxaline (VIa), 2-acylquinoxaline (VI-b), 3-alkyl-3, 4-dihydro-2-quinoxalinecarbonitrile (VIc), 3-alkyl-2-quinoxalinecarbonitrile (VIc'), and 1-alkyl-2 (1H)-quinoxalinone (VId) together with 2, 2' : 3', 2"-terquinoxaline (VIi), in very small yields. The reaction of VII-0 with phenylmagnesium bromide and methylmagnesium iodide in benzene gave only d type of the compound (1-phenyl-(VIId-1), and 1-methyl-4 (1H)-cinnolinone (VIId-5)), and did not isolate other type of the compound. These, a, b, and c type of the compounds were expected reaction products, and other, c', d, e, f, g, and h type of the compounds were unexpected products. Especially, e type of the compound was the product peculiar to the Grignard reaction of V-0, and d type of the compound was characteristic product of the Grignard reactions of the cyanobenzodiazines except 4-quinazolinecarbonitrile (IV-0) giving only a type of the compound. The possible mechanisms of the formations of a, b, c, c', d, and e type of the compounds were proposed.View full abstractDownload PDF (1154K) -
SHIKIFUMI KITAZAWA, MASAHIRO ISHIZU, KEIKO KIMURA1977 Volume 25 Issue 4 Pages 590-600
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffects of surfactants on salicylamide absorption was investigated from the view point of the transmucosal fluid movement using the regular in situ recirculation perfusion technique with the rat small intestine. Surfactants used were polysorbate 80, Pluronic F 68 and Pluronic L 64, and they were dissolved in perfusates in appropriate concentrations. To obtain an accurate ratio of the fluid movement in the presence of surfactants, the cylinder method was developed originally in our laboratory, and validity of the method was demonstrated. Based on the results obtained concerning the effect of surfactants on the drug absorption, the effect of the surfactant on the transmucosal fluid movement was apparently demonstrated. Since extent of the affection was unnegligible, it was suggested that the factor of the transmucosal fluid movement should be taken into considerations as well as the effect of the entrapment of the drug in micelle of the surfactant when the effect of the surfactant on drug absorption would be studied. However, the mode of the affection was different from those brought about by osmotical change, and the surfactant inhibited only in the process of fluid absorption. Based on the difference in nature, the "water-molecule-holding"effect of the surfactant was considered and discussed.View full abstractDownload PDF (1341K) -
SHIKIFUMI KITAZAWA, IKUO JOHNO1977 Volume 25 Issue 4 Pages 601-610
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of increased glucose concentration in blood on the glucose effect proposed in our previous papers were studied with sulfisoxazole, metoclopramide, and sulfanilamide using the in situ recirculating perfusion method with perfusion solution having three different tonicities which were adjusted to hypertonic, isotonic, and hypotonic with sodium chloride or glucose. To achieve the purpose, alloxan-induced diabetic rats were introduced in the present study. No effect of the increase of glucose concentration in blood in the diabetics on the glucose effect was found, since the regression lines representing the relation between the transmucosal fluid movement and the drug absorption with the controls were overlapped to each other with those of the diabetics in both of the media. Simultaneously, the effects of diabetes on the transmucosal fluid movement and the absorption of the drugs were examined. The fluid movement and the absorption of the drugs in the diabetics were always significantly greater than in the controls in all of the experimental conditions. It is reasonable to understand that the increased drug absorptions might be based on only the increment in the transmucosal fluid inflow.View full abstractDownload PDF (1199K) -
HIDEO SETO, KOJI HAYASHI, HIROSHI MITSUHASHI1977 Volume 25 Issue 4 Pages 611-616
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new polyoxypregnane derivative, 12β-O-acetyltomentogenin, was isolated from the stem of Marsdenia tomentosa. A hypothetical biogeneticf pathway of polyoxypregnane derivatives is proposed from their ester linkages.View full abstractDownload PDF (618K) -
ICHITOMO MIWA, JUN OKUDA, KAZUO MAEDA, SHUNICHI UMEDA, AKIRA SAITO, KA ...1977 Volume 25 Issue 4 Pages 617-623
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMutarotase activity in the serum and urine of normal subjects and patients with known renal disease was determined with our mutarotase assay using an oxygen electrode and β-D-glucose oxidase. The activities of alkaline phosphatase and lactate dehydrogenase in serum and urine were also determined. Mutarotase activity was found to be present in the human urine. Elevated urinary mutarotase levels were observed in 7 of the 8 patients with nephrotic syndrome. Urinary levels of two other enzymes were also raised in the same case. Any marked elevation of serum mutarotase, alkaline phosphatase, and lactate dehydrogenase levels was not observed. Urinary mutarotase activity was related to the clinical state of patients with nephrotic syndrome.View full abstractDownload PDF (757K) -
YOSHIHIRO NISHIKAWA, KIMIHIRO YOSHIMOTO1977 Volume 25 Issue 4 Pages 624-631
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA homologous series of 1-O-acyl-D-glucopyranoses (acyl=caproyl, lauroyl, myristoyl, palmitoyl, or stearoyl) were obtained as the anomeric mixtures by condensation of the appropriate fatty acid chlorides with 2, 3, 4, 6-tetra-O-benzyl-α-D-glucopyranose, followed by catalytic hydrogenation : the α anomers were predominant in all the products. Their gas-liquid chromatographic and thin-layer chromatographic behaviors were examined to establish the linear relations of log rtR or Rf values to the acyl chain-lengths. From the anomeric mixtures, their α anomer components were isolated as crystallines by repeated recrystallization. Column chromatographic separation of the acetylated anomeric mixtures furnished the pure acetates of both anomers. The infrared nuclear magnetic resonance and mass spectral features were compared between the pairs of anomers.View full abstractDownload PDF (928K) -
YOSHIKAZU OKA, MICHIO MOTOHASHI, HIROSADA SUGIHARA, OSAMU MIYASHITA, K ...1977 Volume 25 Issue 4 Pages 632-639
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Amino-5, 6-dihydroxy-1, 2, 3, 4-tetrahydro-1-naphthalenol (1), 5, 6-dihydroxy-2-methylamino-1, 2, 3, 4-tetrahydro-1-naphthalenol (2) and 5, 6-dihydroxy-2-isopropylamino-1, 2, 3, 4-tetrahydro-1-naphthalenol (3), which are conformationally rigid derivatives of noradrenaline, adrenaline and isoproterenol respectively, were synthesized from 2-amino-5, 6-dimethoxy-3, 4-dihydro-1 (2H)-naphthalenone (15) prepared by several modifications of the known procedures. The reduction of 1-carbonyl group into hydroxy group at the final step of the syntheses showed unsatisfactory stereoselectivity affording mixtures of 1, 2-cis and 1, 2-trans derivatives. Each cis and trans isomer of 2 (2-cis and 2-trans) was obtained by a sequence of reactions employing 5, 6-dibenzyloxy materials via cis-and trans-2-(N-benzyl-N-methylamino)-5, 6-dibenzyloxy-1, 2, 3, 4-tetrahydro-1-naphthalenol (26-cis and 26-trans).View full abstractDownload PDF (1046K) -
HIROTERU SAYO, AYAKO UEDA1977 Volume 25 Issue 4 Pages 640-646
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAnodic oxidation of benzenesulfon-p-anisidide (I), benzenesulfon-p-toluidide (II), and N-methylbenzenesulfon-p-anisidide (III) were investigated by cyclic voltammetry and controlled potential electrolysis at a glassy-carbon anode in acetonitrile. I showed a single anodic wave in the absence of pyridine, and three anodic waves in the presence of pyridine. On electrolysis of I in the absence of pyridine, p-benzoquinone and benzenesulfonamide were formed. On electrolysis of I in the presence of pyridine, N, N'-dibenzenesulfonyl-N-(4'-methoxyphenyl)-5-methoxy-o-phenylenediamine (IV) and 1-(2-benzenesulfonamido-5-methoxyphenyl) pyridinium perchlorate (V) were obtained. Anodic oxidation of II in acetonitrile containing excess of pyridine gave N, N'-dibenzenesulfonyl-N-(p-tolyl)-5-methyl-o-phenylenediamine (VI) and N, N'-dibenzenesulfonyl-5, 5'-dimethyl-2, 2'-biphenyldiamine (VII). The formation of VI and VII was interpreted in terms of one-electron transfer followed by dimerizations of the free radical of II. On electrolysis of III in the presence of pyridine, 1-(N-methyl-3-benzenesulfonamido-6-methoxyphenyl) pyridinium perchlorate (VIII) was formed as the main product. The position of pyridination, which was ortho to the methoxy-group, was explained on the basis of steric factors.View full abstractDownload PDF (777K) -
YASUO MATSUSHITA, HIDEAKI UMEYAMA, IKUO MORIGUCHI1977 Volume 25 Issue 4 Pages 647-652
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSZ protein was purified from the rabbit and rat liver by fractionation with ammonium sulfate. The physico-chemical properties of Z protein was studied by SDS (sodium dodecyl sulfate) polyacrylamide gel electrophoresis, polyacrylamide gel electrofocusing, amino acid analysis, and sedimentation analysis. The molecular weight was determined to be 1.2×104 by gel filtration on Sephadex G-75 and 1.1×104 by SDS-polyacrylamide gel electrophoresis, and also 8872 and 8639 from amino acid analysis with the rabbit and rat liver, respectively. Z protein lacked tyrosine and tryptophan residues, and had an absorption maximum at 260-270 nm. The isoelectric point was at pH7.0. The sedimentation coefficient of Z protein was ca. 0.7S at a concentration of 0.04-0.06%. Physical and chemical properties of rabbit and ratliver Z protein were closely alike.View full abstractDownload PDF (689K) -
MAMORU SUGIURA, KAZUYUKI HIRANO, SHIRO IINO, HIROSHI SUZUKI, TOSHITSUG ...1977 Volume 25 Issue 4 Pages 653-656
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAlkaline phosphatases (orthophosphoric monoester phosphohydrolase, E.C. 3. 1. 3. 1) from human placenta and intestine are activated by Mg2+, but inhibited by Zn2+. In these respects, the enzymes are different from the human biliary, bone, liver and kidney enzymes, which are much activated by Mg2+ and Zn2+. At pH 10.5, the Km of enzymes and enzymes inhibited by inorganic phosphate are not modified by Mg2+. These results suggest that the activation by Mg2+ proceeds through a binding of Mg2+ with other part of the active site of alkaline phosphatase. It was also found that the activity of alkaline phosphatases was remarkably influenced by binding metals, and Zn2+ and Mg2+ contents in both enzymes were 4 g-atoms/mole and 3-5 g-atoms/mole, respectively.View full abstractDownload PDF (548K) -
ISAO KITAGAWA, MASAYUKI YOSHIKAWA, KWANGSIK IM, YUJI IKENISHI1977 Volume 25 Issue 4 Pages 657-666
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (1187K) -
SEISHI TSUCHIYA, MITSURU HIURA, HIDEO MATSUMARU1977 Volume 25 Issue 4 Pages 667-674
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo investigate the effect of the amount of a base on the absorption of drugs from the rectum, amount of rectal fluid and distribution region of a drug in the rectum after administration of a suppository were determined. The distribution region of a drug in the rectum increased in proportion to the volume of suppository, both in PEG and cacao butter base, The rectal fluid increased with increasing volume of the PEG base, but concentration of the base in rectal fluid was always about 30%, independent of the base volume, at 2 hr after administration. On the other hand, there was no detectable amount of the fluid but a little mucus in the rectum after administration of cacao butter suppository. The results of blood concentration studies showed that both the rate and extent of absorption of sparingly soluble sulfonamides were enhanced by the increasing amount of PEG and cacao butter base. The absorbability of water-soluble sulfonamide was reduced by the increased volume of PEG base, and a better absorbability of a soluble sulfonamide was obtained from cacao butter than from PEG base. The results of in vitro membrane permeation experiment with isolated gut segments served sufficiently to explain the influence of the amount of base on in vivo rectal absorption of sulfonamides. From the results of in vivo and in vitro experiments, it was concluded that rectal absorption of sulfonamides from increased base volume of suppository depended mainly on the increment of the distribution area, that is, absorption area in rectum.View full abstractDownload PDF (863K) -
MASATO YASUHARA, YUJI MIYOSHI, ATSUKO YUASA, TOSHIKIRO KIMURA, SHOZO M ...1977 Volume 25 Issue 4 Pages 675-679
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAbsorption characteristics of cephalosporins were investigated using in situ recirculation technique. Cephalexin as a fairly well absorbed cephalosporin, and cefazolin as a poorly absorbed one were selected as model compounds. Absorption of cephalexin was much faster in its isoelectric region than in alkaline pH. The pH-absorption profile was not consistent with the pH-partition behavior. The absorption of cephalexin was as much as 4.6 times of cefazolin. This difference could not be explained by the pH-partition hypothesis. The surface activities of cephalosporins were investigated and their contributions to the absorption characteristics were little. The transfer rate of cephalosporins from aqueous lecithin liposome dispersion was investigated. The membrane transfer rate of cephalexin was markedly faster than cefazolin and similar result was obtained when liposome was prepared from rat intestinal total lipids. The pH-profile of the transfer rate of cephalexin across the lipid bilayers was similar to the pH-absorption profile. It is suggested that liposomes prepared from total lipids of the intestine as well as lecithin liposomes are suitable and efficient models for investigation of the transfer of these drug molecules across the intestinal membrane.View full abstractDownload PDF (696K) -
SHOJI AWAZU, TAKAYOSHI OGUMA, TATSUJI IGA, MANABU HANANO1977 Volume 25 Issue 4 Pages 680-689
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRoute dependence of area under blood (or plasma) concentration curve (AUC) of drug, or first-pass effect was considered based on a generalized perfusion model where drug is supposed to be disposed in liver and kidney. The results verified the Gibaldi's equation based on a three compartment model to describe the route dependence with hepatic blood flow and hepatic clearance. From this consideration, the equation to described and to predict the dose dependence of AUC with urinary excretion and only one blood concentration at a steady state during a constant infusion was proposed and verified experimentally. And further the correspondence of the generalized perfusion model to a multi-compartment mammillary model for AUC was discussed and the equation for the route dependence was proposed in the case in which drug circulates through enterohepatic system and is disposed in small intestine as well as in liver and kidney.View full abstractDownload PDF (876K) -
ISAMU HORIKOSHI, NORIAKI TAKEGUCHI, MAGOTOSHI MORII, KEN HAYASHI1977 Volume 25 Issue 4 Pages 690-694
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe recompression time dependencies of dynamic loss energy and of the maximum displacement of the upper punch on sorbed or hydrated and anhydrous three compounds of potato starch, dicalcium phosphate and glucose were studied. In every case of our experiments, a linear relationship was found to exist between dynamic loss energy and the maximum displacement of the upper punch. The gradient of the linear relationship expresses an amount of heat generation per unit viscous deformation (J/mm) in recompression and can be utilized as a parameter of solid medicament to evaluate its tablet compressibility. The values of those gradients were much influenced by the sorbed water in potato starch, but a little by the water of hydrated form in dicalcium phosphate and glucose.View full abstractDownload PDF (646K) -
MASATOSHI YAMATO, KUNIKO HASHIGAKI, ETSUKO HONDA, KOICHI SATO, TAKAJI ...1977 Volume 25 Issue 4 Pages 695-699
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn the basis of the previous findings, relationship between the structure and sweet taste was examined by modification of the ethylene unit (B moiety) of β-(3-hydroxy-4-methoxyphenyl) ethylbenzene (1), by application of the theory of bioisosterism : N-Benzyl-3-hydroxy-4-methoxyaniline (2), 3-hydroxy-4-methoxybenzyl phenyl sulfide (4), and phenyl 3-hydroxy-4-methoxythiobenzoate (5) were synthesized. The synthesis of 3-hydroxy-4-methoxybenzyl benzoate (7) was attempted to clarify the effect of elimination of the methylene in 4-position of 8-desoxyphyllodulcin on sweet taste. As modification of 8-desoxyphyllodulcin, related lactone and lactam derivatives were synthesized. 1) Lactone derivatives ; 2-(3-hydroxy-4-methoxyphenyl)-1, 3-benzodioxan-4-one (8), and 2-(3-hydroxy-4-methoxyphenyl)-1, 3-benzothioxan-4-one (9). 2) Lactam derivatives ; 2 (3-hydroxy-4-methoxyphenyl)-2, 3-dihydroisocarbostyril (10), 2-(3-hydroxy-4-methoxyphenyl)-2, 3-dihydro-1, 3-benzoxazin-4-one (11), 2-(3-hydroxy-4-methoxyphenyl)-2, 3-dihydro-1, 3-benzothiazin-4-one (12), 2-(3-hydroxy-4-methoxyphenyl)-4-(3H)-1, 2-dihydroquinazolinone (13), and 2-(3-hydroxy-4-methoxyphenyl) isocarbostyril (14). Additionally, a lactam derivative related to phyllodulcin ; 8-hydroxy-3-(3-hydroxy-4-methoxyphenyl)-3, 4-dihydroisocarbostyril (15), was synthesized in order to examine the effect of a hydroxyl group in 8-position on sweet taste. The compounds 2, 4, 8, and 9 had a strong sweet taste, and the compound 15 had a faint sweet taste ; while the compounds 5, 7, 10, 11, 12, 13, and 14 were all tasteless. Based on these facts, the delicate relationship between the molecular structure and sweet taste was discussed.View full abstractDownload PDF (662K) -
MASATOSHI YAMATO, KUNIKO HASHIGAKI, AKIKO TSUKIOKA, TAKAJI KOYAMA1977 Volume 25 Issue 4 Pages 700-705
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSStructural modification of the 3-hydroxy-4-methoxyphenyl moiety (C moiety) of β-(3-hydroxy-4-methoxyphenyl) ethylbenzene (1), which constitutes an essential part of phyllodulcin molecule, was attempted to clarify the relationship between the structure and sweet taste. The 4-methoxyl group of 1 being replaced with higher homologous alkoxyl groups such as an ethoxyl and a propoxyl group, the level of sweetness of these homologs was found to decrease with increasing number of methylenes in the alkoxyl group. β-(3-Hydroxy-4-methoxycyclohexyl) ethylcyclohexane (8) synthesized by reduction of both aromatic rings of 1 had a bitter taste. Aliphatic derivatives of 1 corresponding to the structure with the aromatic ring of the C moiety opened at the dashed line through a and b as shown in Table II, 9, 10, 11, 12, 13, 14, and 15 were synthesized. All of these compounds had a bitter taste except tasteless 15.View full abstractDownload PDF (822K) -
MASATOSHI YAMATO, KOICHI SATO, KUNIKO HASHIGAKI, TAKAJI KOYAMA1977 Volume 25 Issue 4 Pages 706-713
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSStructural modification of the phenyl moiety (A moiety) of β-(3-hydroxy-4-methoxyphenyl) ethylbenzene (I), which constitute an essential part of phyllodulcin molecules, was attempted to make the relationship between structure and sweet taste clearer. Twenty-four derivatives of A moiety of I were synthesized, the compound (II, IV, V, VI, X, XXII, XXIII, and XXVI) revealed sweet taste and the other compounds were tasteless. On the basis of these data, the taste of these compounds were discussed in connection with the stereochemical hindrance effect of substituents.View full abstractDownload PDF (852K) -
KAZUTAKE SHIMADA, YOUICHI FUJII, ETSUKO YAMASHITA, YURIKO NIIZAKI, YUK ...1977 Volume 25 Issue 4 Pages 714-730
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe isolation and characterization of the cardiotonic steroid constituents in the skin of the Japanese toad, Bufo vulgaris formosus BOULENGER, has been carried out. Three new types of bufotoxins in which the succinoyl, adipoyl, and pimeloyl groups are displaced for the suberoyl residue of the so-called"bufotoxin, "were separated and identified. In addition, the occurrence of bufogenin 3-sulfates and analogous conjugates of cardenolide named cardenobufotoxin was also demonstrated. The ethanolic extract of the skin obtained from 1800 toads was separated by chromatography on Amberlite XAD-2 resin, silica gel, and Sephadex LH-20, followed by highperformance liquid chromatography to provide new cardiotonic steroid conjugates. The structures of these substances were elucidated to be resibufogenin 3-succinoylarginine ester (Id), gamabufotalitoxin homologs (IIg, IIk, IIn, IIp), bufalitoxin homologs (IIIc, IIIe, IIIg, IIIi), cinobufotoxin homologs (IVc, IVe, IVg, IVl), arenobufotoxin (Vd), cinobufotalitoxin (VIb), cardenobufotoxins (VIIId, VIIIf), bufogenin 3-sulfates (IIq, IIIj, Ve, VIId), and sarmentogenin 3-sulfate (VIIIg) by degradative and synthetic means.View full abstractDownload PDF (2247K) -
TADAKATU SAKAMOTO, YOSHIYASU TERAO, MINORU SEKIYA1977 Volume 25 Issue 4 Pages 731-739
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe have newly synthesized a series of N-[(N-nitrosoarylamino) methyl] succinimides, disclosing their syn and anti equilibria in a state of solution. It has been found that these nitrosoamines are capable of furnishing aromatic diazotates in basic media. By allowing the generating aromatic diazotates to react in situ, azo-couplings and triazene formations have been provided. The nitrosoamines behaved in acidic media to suffer a migration of the nitroso group similarly to the Fischer-Hepp migration.View full abstractDownload PDF (911K) -
HARUAKI YAJIMA, HIROSHI OGAWA, NOBUTAKA FUJII, SUSUMU FUNAKOSHI1977 Volume 25 Issue 4 Pages 740-747
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAmong various dilute sulfonic acids tested, 2 to 4N ethanesulfonic acid in acetic acid or methylenechloride was found suitable as a deprotecting reagent for the acid labile α-amino protecting groups, such as Boc and Z(OMe), which are currently removed by trifluoroacetic acid or dilute hydrochloric acid, since the deprotection occured selectively within 60 minutes at room temperature leaving intact other side chain protecting groups, such as Z, benzyl ester, S-p-methoxybenzyl and NG-p-methoxybenzenesulfonyl groups. This reagent was applied to the synthesis of three model peptides ; Met and Leu-enkephalin and endorphin.View full abstractDownload PDF (1035K) -
YOSUKE OHKURA, KENJI OHTSUBO, KAZUYA KOHASHI, KIYOSHI ZAITSU1977 Volume 25 Issue 4 Pages 748-753
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA fluorometric method is presented for the assay of dopamine-β-hydroxylase activity in human serum. This is based on the enzymatic conversion of β-phenylethylamine under the optimum conditions to phenylethanolamine, which is then oxidized to benzaldehyde and determined fluorometrically by means of the previously established method for selective determination of aromatic aldehydes with 1, 2-diaminonaphthalene. The method is readily performed and is suitable to assay a large number of samples at the same time with 10μl of sample.View full abstractDownload PDF (815K) -
MORIO IKEHARA, TOKUMI MARUYAMA, HIROKO MIKI, YOKO TAKATSUKA1977 Volume 25 Issue 4 Pages 754-760
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS8, 2'-O-Cycloadenosine (I) was attacked by azide ion to give 8-oxy-2'-azide compound (II). The 8-oxy function of II was eliminated by derivatization to inosine (IV), acetylation to give V, chlorination with POCl3 to VI, treatment with sodium methylmercaptide to give 6, 8-bis (methylmercapto) compound (VII), reaction with dimethylamine to give VIII and Raney nickel dethiolation to give N6-dimethyl-2'-amino-2'-deoxyadenosine (IX). The compound VI was thiolated into X and treated with hydrogen peroxide to give 3', 5'-di-O-acetyl-2'-azido-2'-deoxyinosine (XI), which was deacetylated to 2'-azido-2'-deoxyinosine (XII). The compound XI was chlorinated and treated with ammonia to give 2'-azido-2'-deoxyadenosine.View full abstractDownload PDF (815K) -
KATSUHIKO MATSUI, YUKIO KAMEDA, TAKUMI ATSUSAKA, MINAKO HIGAKI, KEIKO ...1977 Volume 25 Issue 4 Pages 761-766
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSLeucine dehydrogenase of Bacillus natto KMD 1126 was purified by ammonium sulfate fractionation, diethylaminoethyl cellulose chromatography, Sephadex G 200 gel filtration, and preparative electrophoresis. The homogeneity of purified enzyme was demonstrated by disc gel electrophoresis. Optimum pH for oxidative deamination was 10.7, whereas it was 9.5 for reductive amination. The molecular weight of the enzyme was 360000 daltons as determined by gel filtration on Sephadex G 200. Nicotinamide adenine dinucleotide (NAD+) in the oxidative deamination and reduced NAD in the reductive amination assay could not be replaced by nicotinamide adenine dinucleotide phosphate (NADP+) or reduced NADP. L-Leucine, L-isoleucine, L-valine, and L-alanine were accepted as substrates but not the following amino acids : L-glutamic acid, L-aspartic acid, L-glutamine, L-asparagine, L-serine, L-threonine, L-cysteine, L-lysine, and D-amino acids. p-Chloromercuribenzoate (PCMB) inactivated the enzyme and it was reversed by cysteine. This enzyme had not antitumor activity on Ehrlich ascites carcinoma bearing mice.View full abstractDownload PDF (749K) -
FUSAKO TAMURA, HIROSHI OGAWA, NOBUTAKA FUJII, HARUAKI YAJIMA, KENJI MI ...1977 Volume 25 Issue 4 Pages 767-774
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn a conventional manner, two octadecapeptides corresponding to the entire amino acid sequences of camel β1 and β2-MSHs were synthesized. Synthetic peptides exhibited the in vitro MSH activities of 5.1×109 and 1.1×109 MSH unit/g, respectively.View full abstractDownload PDF (1098K) -
MIKIO TAKEDA, MASATOSHI KAWAMORI, HIROZUMI INOUE, KATSUYUKI NOGUCHI, S ...1977 Volume 25 Issue 4 Pages 775-783
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs part of a study on the steric aspects of the partial agonist activity of phenylazabicycloalkane analgetics, the title compound (A), a skeletal isomer of the known partial agonist (I), was synthesized. The keto ester (IV) was converted to the lactam (VIII) either by hydrogenation of the oxime (V) or by reductive amination. VIII gave A bearing various substituents. Alternatively, A was obtained from the unsaturated amine (XVI) via the bridged aziridine (XVII). Generally, no discernible analgetic activity was observed for A. However, the two N-methyl compounds (Xf and XIc) exhibited narcotic antagonist activity on the order of I and pentazocine. The simple N-methyl-3-phenylpiperidines (II), a prototype of both I and A, also showed comparable antagonist activity. These results support the idea that the N-methylphenethylamine fragment in I is responsible for its antagonist activity. Replacement of the N-methyl group of Xf by an allyl and a propyl group conferred increased antagonist activity. This shift of the potency parallels that observed for II previously.View full abstractDownload PDF (1111K) -
TOKIO SAITO, TETSUO HIRAOKA1977 Volume 25 Issue 4 Pages 784-791
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of the α-amino acid ester (IV) and the 7-amino-cephalosporin (VIII) with thionyl chloride and triethylamine afforded the sulfenimines (V) and (IX), respectively. 7β-Amino-7α-methoxy-cephalosporin derivative (XVI) was obtained by methoxylation of the sulfenimine (IXb) with methanol in the presence of triethylamine.View full abstractDownload PDF (944K) -
TOKIO SAITO, TETSUO HIRAOKA1977 Volume 25 Issue 4 Pages 792-799
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn treatment of the N, N'-disubstituted sulfamides (III) bearing active hydrogens at α-carbons with thionyl chloride and triethylamine, sulfenimines (II) were obtained. These reactions were also applied to cephalosporins (XI and XIII).View full abstractDownload PDF (915K) -
ISAO KITAGAWA, KWANGSIK IM, YOSHIAKI FUJIMOTO1977 Volume 25 Issue 4 Pages 800-808
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to explore a new cleavage method for an arabinoside or a galactoside linkage which attaches to a triterpenoidal or a steroidal aglycone, a photochemical method has been investigated. It has been found that glycoside linkages in 2'-keto-arabinoside and 2'-keto-galactoside derivatives of triterpenoids and a steroid are cleaved upon photolysis to furnish their aglycones in their oxidized forms. In addition, it has been shown that, through the present photochemical procedure, an arabinoside linkage in ziyu-glycoside II (8), which has been known to give an artifact aglycone upon ordinary acid hydrolysis, is cleaved while its acid-labile moiety in the aglycone part is left unchanged.View full abstractDownload PDF (1077K) -
HARUO SAIKACHI, TOKUJIRO KITAGAWA1977 Volume 25 Issue 4 Pages 809-811
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-Ethoxycarbonyl-3, 4-dimethoxycarbonyl-2-methylfuran (6) was prepared from sulfonium 1-ethoxycarbonylacetonylide (1) with dimethyl acetylenedicarboxylate (2). It has been made clear by separate synthetical method that the reaction occurred with, 1.3-shift of the acetyl group of the ylid compound (1).View full abstractDownload PDF (435K) -
TAKEKI OKUMOTO, HIROSHI IMAMURA1977 Volume 25 Issue 4 Pages 812-814
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of several compounds on ultraviolet light-induced unscheduled desoxyribonucleic acid (DNA) synthesis and semiconservative DNA synthesis were examined in rat ascites hepatoma, AH-44 cells. The compounds used did not inhibit unscheduled DNA synthesis as much as or more than semiconservative DNA synthesis. Only improsulfan had a tendency to inhibit unscheduled DNA synthesis to a greater extent than semiconservative DNA synthesis.View full abstractDownload PDF (469K) -
KAZUHIKO HANAI, TAKACHIYO OKUDA1977 Volume 25 Issue 4 Pages 815-816
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA convenient method for the preparation of methanesulfonyl chloride-d3 is described. The procedure consists of the anhydrous chlorination of dimethyl sulfoxide-d6 with chlorine and the aqueous chlorination. Methanesulfonyl chloride-d3 was obtained in a 52% yield, and a small amount of dimethyl sulfone-d6 was also isolated. Trichloromethyl methyl sulfide (-d3) was found to be one of the intermediates in this reaction.View full abstractDownload PDF (427K) -
Cleavage of C-O Bonds of Iminoethers and Methyl Hydroxamates with Grignard Reagents and ButyllithiumAKIHIRO OHTA, SAWAKO MASANO, EIKO MAEDA, TOSHIKO OHWADA, YASUO AKITA, ...1977 Volume 25 Issue 4 Pages 817-821
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSC-O bond in some cyclic iminoethers and methyl hydroxamates were cleavaged by methylmagnesium iodide and butyllithium in a good yield. This reaction was applied to the cleavage of the C-O bond of 4-methoxy-2, 3-dihydrofuro [2, 3-b] quinoline to give 4-hydroxy-3-propylcarbostyril. By the reaction of 3, 6-diisobutyl-1-methoxy-2-oxo-1, 2-dihydropyrazine with methylmagnesium iodide, neoaspergillic acid was obtained.View full abstractDownload PDF (663K) -
KENICHIRO MINEGISHI, MUTSUO OSAWA, TSUTOMU YAMAHA1977 Volume 25 Issue 4 Pages 821-825
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPercutaneous absorption of α-olefin sulfonate (AOS) was investigated in rats by using 14C-labeled compound. The solution of 14C-AOS was applied to the dorsal skin under various conditions : (a) the intact skin dried naturally after application, (b) the intact skin wiped off 0.5 hr after application, (c) the intact skin wiped off 1.5 hr after application, (d) the intact skin with a plastic cup containing 14C-AOS solution and (e) the damaged skin without the stratum corneum dried naturally after application. When rats were applied with 0.5 ml of a 0.2% solution of 14C-AOS under the condition of (a), the recoveries of radioactivity were 0.33% in the urine, 0.08% in the bile and 0.21% in the main organs at 24 hr after application. It was thus estimated that the total amount absorbed through the skin was about 0.6% of the applied dose. Comparing the results obtained under the conditions of (a), (b) and (c), the percutaneous absorption of 14C-AOS applied on the skin was almost finished by 1.5 hr after application. The excretion of radioactivity into the urine and bile was approached to the highest rate around 3-6 hr, then gradually decreased, and continued even 70-90 hr after application. When a 0.02% solution of 14C-AOS was always in contact with the skin under the condition of (d), a small amount of the surfactant was continuously absorbed from the skin. On the other hand, when the skin was damaged and 14C-AOS was applied on it under the condition of (e), a greater amount of radioactivity was excreted into the urine and bile, and the recoveries were 36.26% in the urine, 1.83% in the bile and 12.28% in the main organs 30 hr after application, being about 50% in total.View full abstractDownload PDF (686K) -
HIDENARI SHIGEMATSU, SHIGERU YAMANO, HIDETOSHI YOSHIMURA1977 Volume 25 Issue 4 Pages 825-830
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFollowing the previous study on deethylation of p-nitrophenetole with rabbit liver microsomes, demethylation of p-nitroanisole was analogously investigated, using reduced nicotinamide adenine dinucleotide (NADH), reduced nicotinamide adenine dinucleotide phosphate (NADPH) and NADH plus NADPH as the cofactor. It was found that this reaction proceeded well with NADH as well as NADPH, and this NADH-dependent demethylation was different from those of other two systems. For example, optimum pH was 6.0 in the NADH system, but was 7.4 in the NADPH or NADH plus NADPH system, and the reaction was inhibited by CO in the NADPH or NADH plus NADPH system, but not in the NADH system. Furthermore, KCN did not inhibit the demethylation in any one of three systems at 10-4M. These results were just the same as obtained in the deethylation of p-nitrophenetole and suggested also a possible involvement of a new type of NADH-dependent oxygenase which was different from cytochrome P-450 and cyanidesensitive factor, in the demethylation of p-nitroanisole with rabbit liver microsomes. The NADPH-and NADH plus NADPH-dependent demethylations, on the other hand, were assumed to be catalyzed by the enzyme system involving cytochrome P-450.View full abstractDownload PDF (792K) -
REIMEI MOROI, KENJI ONO, TADASHI SAITO, TAKESHI AKIMOTO, MITSUJI SANO1977 Volume 25 Issue 4 Pages 830-835
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe metabolic pathways of budralazine were studied in vivo and in vitro experiments and characterized as follows ; 1) 3-methyl-s-triazolo [3, 4-a] phthalazine (M-1), one of the major metabolites of budralazine, was mainly biotransformed via 1-hydrazinophthalazine. 2) s-triazolo [3, 4-a] phthalazine (M-3) was also biotransformed via 1-hydrazinophthalazine. 3) Experiments using liver preparations of rat were also discussed briefly.View full abstractDownload PDF (630K) -
TERUAKI YUZURIHA, KOUICHI KATAYAMA, SHINZABURO OHTAKE1977 Volume 25 Issue 4 Pages 836-838
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAutoradiograms of rats following intravenous injection of 125I-labeled lysozyme can be taken to support indirectly the effectiveness and usefulness of lysozyme as a therapeutic agent for chronic sinuitis.View full abstractDownload PDF (629K) -
SEIICHI INAYAMA, YUKIKO TOKUNAGA, EIKICHI HOSOYA, TERUO NAKADATE, TETS ...1977 Volume 25 Issue 4 Pages 838-840
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-Carboxymethylmethamphetamine (III) has been synthesized directly from methamphetamine (I) and through a new route starting from ephedrine (IV). This new hapten was conjugated with BSA and the antiserum for I was prepared by immunization of rabbits with the conjugate (VIII). The production of the antibody for I was confirmed by the ring test and Ouchterlony method.View full abstractDownload PDF (458K) -
SEIICHI INAYAMA, YUKIKO TOKUNAGA, EIKICHI HOSOYA, TERUO NAKADATE, TETS ...1977 Volume 25 Issue 4 Pages 840-842
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe radioimmunoassay for methamphetamine (I) in urine of man has been established by use of the 125I-labelled derivative of N-[3-(p-hydroxyphenylacetylamino) propyl]-methamphetamine (V) in sensitivity of 8.0 ng/100μl. The antigen binding capacity of the antiserum prepared form N-carboxymethylmethamphetamine-BSA (II) was determined by a new method of immunoassay using fluorescence labelled N-(3-dansylaminopropyl) methamphetamine (IV) ("fluoroimmunoassay"). The specificity of the antibody was examined by its cross reaction with several methamphetamine analogues.View full abstractDownload PDF (435K) -
SHINICHIRO SAKAI, NOBUO SHINMA1977 Volume 25 Issue 4 Pages 842-844
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDihydromancunine, a model for a proposed indole alkaloid biosynthetic intermediate, mancunine, was synthesized using a modified Polonovski reaction of desmethylhirsutine N-oxide, which was derived from the indole alkaloid hirsutine.View full abstractDownload PDF (443K) -
IKUNORI SAKAMOTO, KAZUO YAMASAKI, OSAMU TANAKA1977 Volume 25 Issue 4 Pages 844-846
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom leaves of Stevia rebaudiana BERTONI (Compositae), there were isolated three new sweet glycosides, named rebaudioside-C, -D, and -E. Application of 13C NMR spectroscopy as well as chemical evidences led to assign the structure V in Chart 1 to rebaudioside-C.View full abstractDownload PDF (417K) -
JUNICHI GOTO, MASATOSHI HASEGAWA, SETSUKO NAKAMURA, KAZUTAKE SHIMADA, ...1977 Volume 25 Issue 4 Pages 847-849
Published: April 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new method for liquid chromatographic resolution of amino acid enantiomers by the formation of diastereomers has been developed. A chiral reagent used for this purpose, (-)-α-methoxy-α-methyl-1-naphthaleneacetic acid (IIb), was readily prepared by fractionally crystallizing the (+)-α-methylbenzylamine salt. The diastereomers formed from amino acid methyl esters and IIb by the N, N'-dicyclohexylcarbodiimide method were efficiently resolved on the normal phase column.View full abstractDownload PDF (396K)
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