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Volume 30, Issue 1
Displaying 1-50 of 59 articles from this issue
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HIROSHI KASHIWAGI, SABURO ENOMOTO1982 Volume 30 Issue 1 Pages 1-6
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSγ-Ray irradiation of a binary solution consisting of pyridine and methanol caused almost no reaction of pyridine. However, the addition of a catalytic amount of nickel nitrate to this binary solution induced the α-methylation of pyridine in good yield upon γ-ray irradiation at room temperature either in air or in vacuo. This α-methylation gave α-picoline as a major product. The yield of α-picoline increased with increase in the irradiation time at the initial stage of the reaction, reached a maximum (27.8%) at an irradiation duration of between 8 and 10h, and then decreased progressively at greater irradiation times. In addition, the yield of α-picoline at a given irradiation time showed a tendency to increase with increasing amount of the nickel nitrate catalyst or with increasing fraction of methanol in the starting solution. γ-Ray irradiation in the presence of nickel nitrate was also found to induce the catalytic α-methylation of γ-picoline with methanol at room temperature either in air or in vacuo, giving 2, 4-lutidine as a major product in a maximum yield of 8.3%. Further, the demethylation reaction of α-picoline to pyridine and that of 2, 4-lutidine to γ-picoline were also promoted greatly upon γ-ray irradiation at room temperature in air in the presence of both methanol and nickel nitrate.View full abstractDownload PDF (772K) -
YOSHIHARU NISHIMURA, SHUSHI MORITA, JUTARO OKADA1982 Volume 30 Issue 1 Pages 7-16
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree different experiments were carried out in order to estimate the liquid-solid mass transfer coefficient (ks) in a packed bed with porous particles. The experiments were, (A) liquid-phase hydrogenation of maleic acid on Pd-Al2O3, (B) hydrolysis of ethyl acetate on Amberlite 200C, and (C) moment analysis of in-pulse response curve in a packed bed of Amberlite XAD-2. Data were taken at low liquid feed rates and with small particles. The mass transfer factor (jD) which is dimensionless with respect to ks was correlated with the particle Reynolds number (Rep). The obtained values of jD were much lower than those expected from previous correlations obtained from the dissolution of nonporous particles. The results suggested that the effective mass transfer area (as) between liquid and porous particles was less than the geometrical outer surface area of the particles. as was considered to be influenced by the stagnant hold-up and the pore openings.View full abstractDownload PDF (987K) -
HIROSHI KASHIWAGI, SABURO ENOMOTO1982 Volume 30 Issue 1 Pages 17-23
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe numbers of radicals generated in binary powders of glycolic acid and silicaalumina and of potato starch and silica-alumina determined by means of electron spin resonance (ESR) were found to be affected by mechanical energies. For example, the numbers of spins increased with increase in the shaking duration, with increase in the compressive stress, and with decrease in the size of particles. The numbers of radicals were also influenced by the techniques used for mixing the binary powders. An increase in the number of radicals induced by mechanical forces may increase the rates of chemical reactions during the manufacture and storage of drugs.View full abstractDownload PDF (786K) -
MASAMI INOUE, YASUSHI ITOI, SABURO ENOMOTO, NAOYASU ISHIZUKA, HIDEMITS ...1982 Volume 30 Issue 1 Pages 24-27
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCatalytic dehydrogenation of iminodibenzyl to iminostilbene was carried out at 550°C on a binary oxide system of Mn2O3-SnO2. Maximum activity was observed at an Mn2O3-SnO2 ratio of 8 : 2 ; conversion was 40%, selectivity 82%. Mn2O3-SnO2 catalyst dispersed on MgO and modified with K2CO3 gave 80-90% conversion and 82-88% selectivity. The relation between activity and the physical properties of catalysts was studied.View full abstractDownload PDF (508K) -
HITOSHI YAMAGUCHI, FUMIYOSHI ISHIKAWA1982 Volume 30 Issue 1 Pages 28-34
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethylation of 2-chloro-3, 4, 5, 6, 7, 8-hexahydro [1] benzothieno [2, 3-d] pyrimidine (1) gave the 3-methyl derivative as a major product, but benzylation predominantly afforded the 1-substituted product. On the other hand, alkylation of 1 with an α-carbonylalkyl halide predominantly occurred at position 3. The 2-chloro-1-or 3-alkylated compounds were easily hydrolyzed to give the corresponding 1-alkyl-2 (1H)-or 3-alkyl-2 (1H)-one derivatives, which were readily oxidized to the corresponding 3, 4-or 1, 4-dehydrogenated compounds, respectively. The 2-chloro-3-substituted compounds were used for the synthesis of new heterocycles, imidazo [1, 2-a] thieno [2, 3-d] pyrimidine and 2, 3-dihydro-5H-oxazolo [3, 2-a] thieno [2, 3-d]-pyrimidine.View full abstractDownload PDF (879K) -
KAZUE SATOH, TADASHI MIYASAKA, KIICHI ARAKAWA1982 Volume 30 Issue 1 Pages 35-43
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn reaction with sodium salts of such active methylene compounds as ethyl cyanoacetate, malononitrile, ethyl malonate and phenylacetonitrile, thiazolo [3, 2-b] pyridazinium perchlorates (I) furnish anhydro-8-(α, α-disubstituted methylene)-5, 8-dihydrothiazolo [3, 2-b]-pyridazinium hydroxides (IV, V, VI, and VII). On treatment with sodium hydrosulfide as a nucleophile, I affords anhydro-8-mercaptothiazolo [3, 2-b] pyridazinium hydroxide (X). The reaction is initiated by the nucleophilic addition of the reagents at the 8-position, and subsequent oxidation by atmospheric oxygen via radical intermediates gives rise to the ylide compounds.View full abstractDownload PDF (950K) -
MASARU KIDO, IWAO MIURA, YOSHIAKI MANABE, KAZUYUKI NAKAGAWA1982 Volume 30 Issue 1 Pages 44-50
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe molecular structure of procaterol hydrochloride hemihydrate (C16H22N2O3·HCl·1/2H2O) was determined by X-ray diffraction analysis. The crystal is orthorhombic with the space group P22121 and Z=4. The cell dimensions are a=7.247 (2), b=12.491 (8), and c=18.822 (13) A. The structure was solved by a direct method using the MULTAN program and refined by a block-diagonal least-squares method to give a final R-value of 0.069. The N (2')+ cation of the side chain forms two hydrogen bonds with Cl- anion and a water molecule but not with O (3') atom, although O (3')-C (11)-C (12)-N (2') is gauche (53°) with a close intramolecular N (2')-O (3') distance of 2.679 (7) A. It was confirmed by proton magnetic resonance spectroscopic measurements that the molecular conformation found in the crystal is retained in solution as a preferred conformation.View full abstractDownload PDF (696K) -
TOSHIO TANAKA, KIYOSHI BANNAI, TAKESHI TORU, TAKEO OBA, NORIAKI OKAMUR ...1982 Volume 30 Issue 1 Pages 51-62
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo series of 8-acetyl-12-hydroxyalkadienoic acids and 14-hydroxy-9-oxoalkadienoic acids, which can be regarded as 11, 12-and 8, 12-secoprostaglandin E2, were synthesized and evaluated for biological activity on platelet function. Key members of each series, 11, 12-and 8, 12-seco-11-norprostaglandin E2, were found to induce platelet aggregation. This effect was inhibited by preincubation of PRP with prostaglandin I2 but was not inhibited by indomethacin.View full abstractDownload PDF (1420K) -
NORIO KAWAHARA, TSUNEO ITOH, HARUO OGURA, KYOICHIA WATANABE1982 Volume 30 Issue 1 Pages 63-66
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN, N'-Dialkyl-N-[3-methoxy-3-dialkylamino-2-(3-methoxycarbonylpropioloyl) acryloyl] ureas (3) were synthesized by coupling of 1, 3-dialkyl-6-(N-substituted) aminouracils (2) and dimethyl acetylenedicarboxylate (DMAD). Compounds (3) are stable crystalline materials at room temperature, but on heating in DMF, they undergo cyclization, giving rise to the pyrido [2, 3-d] pyrimidine derivatives. These compounds were characterized by 1H-nuclear magnetic resonance (NMR), 13C-NMR, mass spectral and elemental analyses.View full abstractDownload PDF (595K) -
TOSHIAKI MIURA, KUNIHIKO SHIBATA, TAKUJI SAWAYA, MICHIYA KIMURA1982 Volume 30 Issue 1 Pages 67-73
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxygenation reactions of adamantanes with ferrous iron-molecular oxygen in phosphate buffer were investigated and the structures of the products were elucidated. In the reaction of adamantane-1-acetic acid (1a), five oxygenated products, the C (2)-oxo, C (4)-oxo, C (2), C (6)-dioxo, C (4)-ol, and C (3)-ol derivatives, were obtained. Similar oxygenation also occurred in the reaction of adamantane-1-carboxylic acid (2a) to give three products, the C (4)-oxo, C (4)-ol, and C (3)-ol derivatives. The oxy-functionalization of 1a and 2a in 0.5M phosphate buffer (pH 6.8) was found to occur almost quantitatively on addition of an appropriate amount of ferrous iron.View full abstractDownload PDF (887K) -
CHIKARA KANEKO, HARUE FUJII, SHINJI KAWAI, KAZUHIKO HASHIBA, YOSHIO KA ...1982 Volume 30 Issue 1 Pages 74-85
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIrradiation (≥300 nm) of methyl 2-phenyl-3, 1-benzoxazepine-5-carboxylate in an alcohol afforded the Z-isomer of methyl 3-alkoxy-2-(2-benzamidophenyl)-acrylate as the major addition product. In contrast, thermal reaction of the oxazepine with a primary alcohol in the presence of triethylamine led to the exclusive formation of the corresponding E-isomer. The same kinds of Michael addition products were also obtained stereoselectively from 3, 1-benzoxazepines having an acetyl group at the 5-position under these conditions. The interrelation between the stereoisomers obtained from the oxazepine and an alcohol under these two conditions was established by photochemical equilibration, and the stereochemistry of the two isomers was determined by proton magnetic resonance spectroscopy. An explanation is proposed for the observed stereoselectivities in the two kinds (photochemical and thermal) of reactions.View full abstractDownload PDF (1334K) -
TAISUKE ITAYA, HIROO MATSUMOTO, TOMOKO WATANABE1982 Volume 30 Issue 1 Pages 86-90
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of 2', 3', 5'-tri-O-benzoyl-N, N-dimethyladenosine (2c) with methyl iodide in AcNMe2 gave the 3-methyl derivative (3c) as a sole product. Alkaline hydrolysis of 3c afforded the title imidazolecarboxamide (4a), whose hydroxy groups were acetylated selectively with Ac2O-pyridine. Similar methylation of 2', 3', 5'-tri-O-benzyl-N, N-dimethyladenosine (2d) followed by alkaline hydrolysis provided 2', 3', 5'-tri-O-benzyl-4a (4d) in good yield.View full abstractDownload PDF (736K) -
JUTARO OKADA, KOICHI NAKANO, HIROSHI MIYAKE, SHOJI YASUFUKU1982 Volume 30 Issue 1 Pages 91-96
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-(4-Halophenylthiomethyl)-6-alkoxycarbonyluracils (IIa-i) and 5-(4-halophenylthiomethyl)-6-alkylcarbamoyluracils (IVa-p) were prepared from 5-(4-halophenylthiomethyl)-6-ethoxycarbonyluracils (Ia-c). The compounds thus prepared were examined for growth inhibition of L-1210 cells in vitro.View full abstractDownload PDF (618K) -
Chemical Transformation of Tylosin, a 16-Membered Macrolide, and Its Structure-Activity RelationshipHAJIME MATSUBARA, KATSUJI MIYANO, AKIRA NAKAGAWA, SATOSHI OMURA1982 Volume 30 Issue 1 Pages 97-110
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTylosin is a 16-membered macrolide antibiotic used as veterinary antimicrobial agent. In this paper, we describe the structure of a novel condensation product obtained by acidic hydrolysis and alkaline treatment of tylosin, as well as the isolation of the aglycone part, tylonolide 5, 20-hemiacetal, by application of a modified Polonovski reaction to tylosin. Furthermore, we describe syntheses of the intermediates of tylosin biosynthesis and of related compounds, and also the relationship between the structure and antimicrobial activity.View full abstractDownload PDF (1355K) -
KEIJI HEMMI, KIDEKAZU TAKENO, MASASHI HASHIMOTO, TAKASHI KAMIYA1982 Volume 30 Issue 1 Pages 111-118
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of analogs of 3-(N-acetyl-N-hydroxyamino) propylphosphonic acid (FR-900098, Ia) and an analysis of their structure-activity relationship are described. Among them, compounds Ib (FR-31564) and XIIb (FR-32863) have recently been found to be produced naturally by Streptomyces lavendulae. The antibacterial activity of Ib against Pseudomonas species is especially significant.View full abstractDownload PDF (876K) -
NORIO HASHIMOTO, TOYOHIKO AOYAMA, TAKAYUKI SHIOIRI1982 Volume 30 Issue 1 Pages 119-124
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTrimethylsilyldiazomethane (TMSCHN2) easily reacts with various ketones in the presence of boron trifluoride etherate in methylene chloride solution to give chain- or ring-homologated ketones, and can be used as a stable and safe substitute for hazardous diazomethane. The reaction proceeds below 0°C during 1-4h, and permits much more efficient homologation than can be achieved with diazomethane.View full abstractDownload PDF (756K) -
SHUICHI UEDA, SETSUO TAKEDA, ICHIRO YAMAWAKI, JUNICHI YAMASHITA, MITSU ...1982 Volume 30 Issue 1 Pages 125-131
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA hydroxylated metabolite of 1-(tetrahydro-2-furanyl)-5-fluorouracil (FT), 1-(trans-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (trans-3'-OH-FT, VIII) and its isomer, 1-(cis-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (cis-3'-OH-FT, VI), were synthesized and isolated at high purity. As compounds related to FT metabolites, 2, 3'-anhydro-1-(cis-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (2, 3'-anhydro-FT, V), 1-(2, 5-dihydro-2-furanyl)-5-fluorouracil (3', 4'-dehydro-FT, XII) and 1-(5-acetoxytetrahydro-2-furanyl)-5-fluorouracil (5'-AcO-FT, XI) were also synthesized. The antitumor activities of these compounds against sarcoma 180 and L 1210 were examined. The activities of cis-3'-OH-FT (VI) and 2, 3'-anhydro-FT (V) were found to be lower than that of FT. The activity of 5'-AcO-FT (XI) was the same as that of FT. 3', 4'-Dehydro-FT (XII) showed much greater activity than FT.View full abstractDownload PDF (761K) -
YUKINOBU IKEYA, HEIHACHIRO TAGUCHI, ITIRO YOSIOKA1982 Volume 30 Issue 1 Pages 132-139
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new dibenzocyclooctadiene lignans, named (-)-gomisins L1 (6) and L3 (7), (±)-gomisin M1 (8) and (+)-gomisin M2 (9), were isolated from the fruits of Schizandra chinensis BAILL. (Schizandraceae). Their absolute structures were elucidated by means of chemical and spectral studies. The stereostructure of γ-schizandrin (1, dl-form), the plane structure of which had already been suggested by Kochetkov et al. and Liu et al., was also elucidated on the basis of chemical and spectral studies.View full abstractDownload PDF (954K) -
KENICHI YAKUSHIJIN, TOYOHISA TSURUTA, HIROSHI FURUKAWA1982 Volume 30 Issue 1 Pages 140-151
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermal decompositions of methyl 5-[2-(2-azidophenyl) ethyl]-2-furoate (3a), methyl 5-[2-(2-azido-4, 5-methylenedioxyphenyl) ethyl]-2-furoate (3b) and methyl 5-[2-(2-azido-4, 5-dimethoxyphenyl) ethyl]-2-furoate (3c) gave methyl pyrrolo [1, 2-a] quinoline-3-carboxylates (10a-c) ; in the case of 3a, the 4, 5-dihydro product 9 was also obtained. Photochemical decompositions of 3a and 3b in ethanol gave methyl 4, 5-dihydro-1-ethoxypyrrolo [1, 2-a]-quinoline-3-carboxylates (15a, b). In contrast, the cyclization product was not detected from 3c under similar conditions. Methyl 5-(2-azido-4, 5-dimethoxybenzyl)-2-furoate (8) gave 7, 8-dimethoxypyrido-[1, 2-a] indole-1, 2-dione (22) on thermolysis, and on photolysis in ethanol, gave methyl 6, 7-dimethoxy-9H-pyrrolo [1, 2-a] indole-3-carboxylate (23), trans-methyl 3-(6, 7-dimethoxy-3-hydroxy-2-quinolyl) acrylate (25) and 22. The pathways of these of these reactions are discussed.View full abstractDownload PDF (1349K) -
SHOETSU KONNO, MASAAKI YOKOYAMA, AKIKO KAITE, IKUKO YAMATSUTA, SHIGERU ...1982 Volume 30 Issue 1 Pages 152-157
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe potassium permanganate oxidation of 3-methylthio-5, 6-diphenyl-as-triazine in the presence of a phase-transfer catalyst afforded 3-methylsulfonyl-5, 6-diphenyl-as-triazine. The 3-sulfonyl-as-triazine readily reacted not only with active methylene compounds but also with methyl or methylene ketones under basic conditions, and 5, 6-diphenyl-as-triazines containing a functionalized carbon substituent at the 3-position were obtained. Similarly, 2-substituted 4, 6-dimethylpyrimidines were synthesized by the nucleophilic substitution of 4, 6-dimethyl-2-phenylsulfonylpyrimidine with various ketones.View full abstractDownload PDF (816K) -
TAMON MORIYA, NAOTO YONEDA1982 Volume 30 Issue 1 Pages 158-166
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethyl 2-isocyano-3-[3 (1H)-indolyl] acrylate (1) was synthesized in 73-75% yield by the reaction of 3-(aminomethylene)-3H-indoles (5) with methyl α-isocyanoacetate (3) in pyridine or dimethylformamide, while the reaction in methanol afforded selectively 2-(aminomethyleneamino)-3-[3 (1H)-indolyl] acrylates (6a-e) in 63-100% yields. The mechanisms of formation of 1 and 6 are discussed. Both 1 and 6a-e were hydrolyzed to N-formyl-α, β-dehydrotryptophan (8) and/or its methyl ester (2).View full abstractDownload PDF (939K) -
TETSUJI KAMETANI, TOSHIO SUZUKI, AKIKO TOMINO, KATSUO UNNO1982 Volume 30 Issue 1 Pages 167-171
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA general method for the stereoselective synthesis of the non-tryptamine components of reserpine and yohimbine via the same compound (6) is described. This common intermediate was readily obtained by Diels-Alder reaction of the furfural derivative (10) with maleic anhydride.View full abstractDownload PDF (605K) -
FUMIO YONEDA, KEISHI NAKAGAWA, AKIRA KOSHIRO, TOSHIO FUJITA, YUKIKO HA ...1982 Volume 30 Issue 1 Pages 172-179
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of 6-(1-methylhydrazino) uracil (I) with phenacyl bromides in methoxyethanol afforded the corresponding 3-aryl-1-methylpyrimido [4, 5-c] pyridazine-5, 7 (1H, 6H)-diones (3-aryl-6-demethyl-4-deazatoxoflavins) (II) and 3-aryl-5, 7-dioxo-1-methyl-1, 4, 5, 6, 7-pentahydropyrimido [4, 3-c] [1, 2, 4] triazines (III). Methylation of II and III with methyl iodide gave the corresponding 3-aryl-4-deazatoxoflavins (IV) and 1, 6-dimethyl-5, 7-dioxopyrimido [4, 3-c] [1, 2, 4] triazines (V). The reaction of IV with m-chloroperbenzoic acid in chloroform gave the corresponding 3-aryl-4, 4a-epoxy-4-deazatoxoflavins (VI). The oxidizing abilities of II toward alcohols were examined in comparison with those of IV from both kinetic and synthetic viewpoints. Treatment of IV with 30% aqueous caustic alkali led to the exclusive formation of 4, 8-dihydro-4-deazatoxoflavins (VII) and 4, 8-dihydro-4-deazatoxoflavin-4-ones (VIII) via intermolecular oxidation-reduction between the initially formed 4-hydroxy-4, 8-dihydro-4-deazatoxoflavins (IX) and unchanged IV. Treatment of VI with 10% aqueous sodium hydroxide gave the 6-aryl-4-hydroxy-2-methylpyridazine-3 (2H)-ones (X).View full abstractDownload PDF (747K) -
MUNEFUMI KANAO, TAKESHI HASHIZUME, YOSHIFUMI ICHIKAWA, KIYOSHI IRIE, Y ...1982 Volume 30 Issue 1 Pages 180-188
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of semi-rigid analogs of phenethylamine was prepared as fixed transoid and cisoid analogs of mebeverine, and tested for spasmolytic activity in vitro. The fixed transoid analogs were more potent than the corresponding cisoid analogs. In this series, tetrahydro-2-napthylamine derivative (2a) which is presumed to take transoid conformation had the most potent activity, and tetrahydroisoquinoline derivatives (2g and 2h) which are presumed to take typical cisoid conformations were less active. These results suggested that the phenethylamine moiety of mebeverine takes the transoid conformation for the manifestation of the spasmolytic activity.View full abstractDownload PDF (898K) -
TAISUKE HOJO, HIROSHI NAKAMURA, ZENZO TAMURA1982 Volume 30 Issue 1 Pages 189-195
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe fluorescence properties of biogenic indole compounds in perchloric acid (PCA) solution were investigated. The indoles gave specific yellow-greenish fluorescence in PCA solution (λex=425 nm and λem=525 nm for 3-substituted indoles ; λex=300 nm and λem=525 nm for 3, 5-substituted indoles) under the optimal conditions. Based on the results of optimization studies for the fluorogenic reaction, two fluorometric methods for the determination of these substituted indoles at the 100 pmol level were developed.View full abstractDownload PDF (739K) -
YASUHIKO MATSUKI, TOMIHARU ITO, SAKAE KOMATSU, TOSHIO NAMBARA1982 Volume 30 Issue 1 Pages 196-201
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe characterization and quantitation of a new urinary metabolite, M2, from rats orally given atenolol, a β-adrenergic blocking drug, are described. 4-(2-Hydroxy-3-isopropylaminopropoxy) phenylglyoxylic acid amide was synthesized as an authentic sample by an unequivocal route. The structure of M2 was definitively established by direct comparison with the synthetic specimen. Determination of M2 in urine was achieved by means of selected ion monitoring (SIM) using [3H6]-atenolol as an internal standard. The amount of M2 excreted in urine was estimated to be 1.04% of the dose.View full abstractDownload PDF (688K) -
HIROSHI HOSODA, KEIKO USHIODA, HIROAKI SHIOYA, TOSHIO NAMBARA1982 Volume 30 Issue 1 Pages 202-205
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to develop specific and sensitive immunoassays, new carboxylated derivatives of androstenedione, 11β-hydroxyandrostenedione, adrenosterone, progesterone, 17α-hydroxyprogesterone, corticosterone, 11-deoxycorticosterone and 21-deoxycortisol were synthesized. The preparation of the 4-carboxymethylthio and 4-carboxyethylthio derivatives of the Δ4-3-ketosteroids was carried out by base-catalyzed ring opening of the 4, 5-epoxides with mercaptoacetic acid and mercaptopropionic acid, respectively. The N-succinimidyl esters of these carboxylated steroids were also prepared.View full abstractDownload PDF (623K) -
MICHINAO MIZUGAKI, YOKO ITO, TOSHIAKI HOSHINO, TAKAYUKI SHIRAISHI, HIR ...1982 Volume 30 Issue 1 Pages 206-213
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-Acetylcysteamine and coenzyme A esters of cis-2-alkenoic acids have been found to undergo isomerization to the corresponding trans-isomers during their preparation by the mixed anhydride method and also during their alkaline hydrolysis. The isomerization might proceed by interaction of the free thiol group and the cis-double bond of 2-alkenoic thiol esters. The use of pyridine as a base and three or more equivalents of the mixed anhydride to the thiol compound prevented the formation of the trans-isomer. Addition of hydrogen peroxide during alkaline hydrolysis also prevented the isomerization completely.View full abstractDownload PDF (770K) -
MITSUO NAKAGAWA, HAYAO KOBAYASHI, MIEKO KATSUYA, NORIKO TAKADA, SHOJI ...1982 Volume 30 Issue 1 Pages 214-218
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe lecithin-cholesterol acyltransferase activity in rat serum as well as that in human plasma was examined by using sonicated dispersions of lecithin and cholesterol mixtures as substrates. When dispersions with molar ratio of 1.2 and 5.9 were used as substrates, the acyltransferase activity in rat serum, in contrast to that in human plasma, was greater with the substrate dispersion having a molar ratio of 1.2 than with that of 5.9. In addition, the acyltransferase activity in rat serum with the dispersion having a molar ratio of 0.9 was inhibited upon addition of increasing amounts of lecithin, but that in human plasma for the same dispersion was stimulated and the maximum acyltransferase activity was obtained at a molar ratio of approximately 7. On the basis of these results, the inhibitory actions of organophosphate pesticides on the acyltransferase and cholinesterase in rat serum were investigated. The acyltransferase activity in rat serum was inhibited by the addition of 1×10-3M dimethyldichlorovinylphosphate (DDVP) and methylparathion. The decreased acyltransferase activity in rat serum was not restored by the addition of 1×10-3M 2-pyridine aldoxime methiodide (PAM). Similarly, cholinesterase activity in rat serum was almost completely inhibited by the addition of 1×10-5M DDVP. However, the decreased cholinesterase activity was restored by the addition of 1×10-3M PAM. In addition, the acyltransferase and cholinesterase activities in serum obtained from rats administered DDVP (35 mg/kg body) in vivo were inhibited to approximately 83-87% and 35-37% of those in control rat serum, respectively.View full abstractDownload PDF (657K) -
YOSHIYUKI KIMURA, MICHINORI KUBO, KIMIYO KUSAKA, TADATO TANI, MASAYUKI ...1982 Volume 30 Issue 1 Pages 219-222
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of oral administration of flavonoid components of Scutellariae Radix on serum and liver lipid levels of rats treated with ethanol were investigated. It was found that wogonin reduced serum triglyceride level, and that baicalein and baicalin, the major components of the drug, decreased total cholesterol, free cholesterol and triglyceride contents in the liver. Baicalein increased high density lipoprotein-cholesterol (HDL-ch) in the serum of the ethanol-treated rats. In addition to these in vivo experiments, the actions of wogonin, baicalein and baicalin on catecholamine-induced lipolysis in isolated fat cells were investigated. It was found that the three flavones inhibited noradrenaline-induced lipolysis in isolated fat cells. The relationship between these in vivo and in vitro experiments is discussed.View full abstractDownload PDF (519K) -
SATOSHI OMURA, NORIAKI SADAKANE, HAJIME MATSUBARA1982 Volume 30 Issue 1 Pages 223-229
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to clarify the later stages of tylosin biosynthesis, the biotransformation of tylosin-related compounds to tylosin was examined in a tylosin-producing strain, Streptomyces fradiae KA-427, with the aid of cerulenin, which is an inhibitor of fatty acid and polyketide biosynthesis. Protylonolide (9), 5-O-mycaminosylprotylonolide (11), deepoxycirramycin A1 (12), 20-deoxy-5-O-mycaminosylrelonolide (13), 5-O-mycaminosyltylonolide (3) and demycarosyltylosin (2) were bioconverted to tylosin. However, 23-hydroxyprotylonolide (10), 20-deoxydemycarosylrelomycin (14) and 20-deoxy-23-O-mycinosylrelonolide (16) were bioconverted not to tylosin, but to 20-deoxyrelomycin (15). Thus, the biosynthetic pathway via compounds 11 and 3 is proposed.View full abstractDownload PDF (688K) -
TOSHIYUKI FUJIOKA, KAZUTAKA TANIZAWA, YUICHI KANAOKA1982 Volume 30 Issue 1 Pages 230-236
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAcyl trypsins containing the 1-dimethylaminonaphthalene-5-sulfonyl (DNS) fluorophore were prepared in a very specific manner by employing substrates of a new type. The properties of isolated acyl trypsins were spectrofluorometrically analyzed. The deacylation rate of the acyl trypsin, which no longer retains a cationic site-specific group on the acyl group, was enhanced by the addition of alkylammonium ions. This kinetic behavior was shown to be reflected in the fluorescence spectra. These results are discussed on the basis of conformational change of the trypsin active site.View full abstractDownload PDF (754K) -
YOSHIHISA IWAMOTO, ICHIJI MIFUCHI1982 Volume 30 Issue 1 Pages 237-241
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe presence of superoxide dismutase activity was demonstrated in the dialyzed cellfree extracts of lactobacilli which are considered to be obligatory anaerobes or microaerobes. Specific activities of Lactobacillus acidophilus A-28 YIT 0066, L. casei C-16 ATCC 7469, L. arabinosus ATCC 8014, L. casei S-1 YIT 0001 and L. plantarum 11-35 YIT 0101 were about 0.2-0.4 units/mg protein, which are much lower than those of Streptococcus faecalis and Escherichia coli. Activity was rather constant when L. acidophilus A-28 was grown aerobically in the MRS medium containing glucose, mannitol or sorbitol, though the cells grown with mannitol or sorbitol consumed more oxygen than the cells grown with glucose. Activity of the cells grown anaerobically may have constitutively definite activity sufficient for cell survival on exposure to aerobic conditions. The superoxide dismutase of lactobacilli is not a cupro-zinc enzyme, since it was not inhibited by 5 mM potassium cyanide.View full abstractDownload PDF (639K) -
HIROSHI NAKAGAWA, YOSHITERU TAKAHASHI, ISAO SUGIMOTO1982 Volume 30 Issue 1 Pages 242-248
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of grinding and drying (removal of water of crystallization) processes on the solid state stability of sodium prasterone sulfate (DHA·SO3Na·2H2O) were studied. As the grinding time was increased, the sample became more unstable. From the study of the thermal behavior of the water of crystallization, it was suggested that the bonding force between the water of crystallization and DHA·SO3Na molecule within the hydrate crystal was weakened by grinding, and water molecules participated in the hydrolysis of DHA·SO3Na more easily. Although DHA·SO3Na was found to be hydrolyzed, the ground DHA·SO3Na·2H2O was more stable under conditions of high humidity than low humidity. This result is very interesting, and it was considered that the bonding force between the water of crystallization and DHA·SO3Na molecule was strengthened in conditions of high humidity. The dehydration of DHA·SO3Na·2H2O resulted in a higher disorder of the crystal structure and water molecules were sufficiently free to participate in a solid state hydrolytic reaction. Therefore, partially dehydrated DHA·SO3Na·2H2O decomposed easily. After almost complete removal of the water of crystallization, the sample was relatively stable, since it contained few water molecules which could participate in hydrolysis. The dihydrate form was the most stable.View full abstractDownload PDF (702K) -
KAZUYA FUKASAWA, MOTOME NISHIDA, RYOHEI ICHIDA, YURIKO KATO1982 Volume 30 Issue 1 Pages 249-256
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRabbits were intravenously coadministered with salicylate and each of various phenylbutazone analogues (oxyphenbutazone, γ-hydroxyphenylbutazone and ketophenylbutazone). After the drug administration, concentrations of salicylate and its metabolites in the plasma and in the urine were determined by using the GLC method. Salicylate elimination from the plasma was suppressed by oxyphenbutazone and ketophenylbutazone, but was not suppressed by γ-hydroxyphenylbutazone. The renal excretion of salicylate was markedly inhibited by each of the phenylbutazone analogues and the amount of salicylurate excreted was relatively increased, whereas that of salicyl glucuronides was insignificantly affected. Phenylbutazone itself slightly depressed the renal excretion of salicylurate.View full abstractDownload PDF (865K) -
NOBUHIRO MURAMATSU, TOSHIMITSU YOSHIOKA, TAMOTSU KONDO1982 Volume 30 Issue 1 Pages 257-265
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSheep hemolysate-loaded artificial red blood cells with different membrane compositions were prepared by making use of the interfacial polycondensation reaction between diamines and terephthaloyl dichloride. When these artificial red blood cells were added to rabbit platelet-rich plasma, the platelets rapidly adhered to the artificial red blood cells and obvious differences were seen in platelet adhesion between cells of different membrane compositions. On the other hand, platelet adhesion was not affected by the membrane composition in the absence of the plasma, suggesting that platelet adhesion is strongly affected by plasma components. Among various substances in plasma, the major components, proteins, could be expected to play an important role in platelet adhesion. Therefore, three kinds of proteins, fibrinogen, γ-globulin and albumin, were chosen as typical plasma components and differences in their adsorption behavior on artificial red blood cells were examined. As a result, it was found that fibrinogen and γ-globulin were adsorbed very rapidly and in large amount on the artificial red blood cells while albumin was very little adsorbed under physiological conditions. It was further found that the rate and amount of protein adsorption were dependent on the membrane composition of the artificial red blood cells. The platelet adhesion was found to be affected by coating of the artificial red blood cells with these proteins, but the results were not consistent with the glycosyl transferase hypothesis. Accordingly, it was considered that the dependence of platelet adhesion on the membrane composition of artificial red blood cells is caused by differences in the complex layers of plasma proteins formed rapidly on the artificial red blood cells.View full abstractDownload PDF (1214K) -
HIROSHI FUJIWARA, SUSUMU KAWASHIMA, SACHIKO OMURA1982 Volume 30 Issue 1 Pages 266-271
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSince the mixing of many kinds of granules is necessary for the manufacture of solid dosage forms, the determination of their mixing limit is very important. Equations to calculate the theoretical mixing degree were obtained by Lacey and Stange for homogenous particles and for particles with a grain size distribution in binary systems. However, it became clear that the theoretical values thus obtained are very different from the experimental ones for the mixing of two kinds of granules with different grain size distributions. Hence, by assuming space filling with target granules of small size and by utilizing the experimental mixing values, new equations were obtained. The resulting theoretical values were in fair agreement with the experimental ones. Thus, it is considered that the mixing degree was affected not only by variation based on the random arrangements of particles, but also by the grain size distributions of the target particles in the mixing of granules with different grain sizes.View full abstractDownload PDF (563K) -
HIROYUKI FUJIMORI, CHIAKI MORIWAKI, SHUICHIRO HAMANO1982 Volume 30 Issue 1 Pages 272-279
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of kallikrein and some autacoids on the transport and uptake of valine in the rat small intestine was examined, in vitro, by the method of sac of everted in testine and by measurement of uptake of valine in the tissue. Kallidin and rat intestinal kallikrein (RIK) stimulated the intestinal transport of valine, like bradykinin and pancreatic kallikrein. Kallidin was more effective than bradykinin or Met-Lys-bradykinin. RIK stimulated the transport significantly when it was added to either the mucosal or serosal side. Moreover, the accumulation of valine into the small intestine was enhanced by bradykinin, and a similar result was obtained by the combined addition of rat pancreatic kallikrein and rat kininogen to the medium. The net mucosa-to-serosa Na+ transport was enhanced by the addition of bradykinin to the serosal side of the everted intestine, and Na+ transport was further increased by adding bradykinin to the serosal fluid and glucose to the mucosal. The net Na+ transport was suppressed by the addition of ouabain in the serosal fluid, but was restored to the normal level by bradykinin. Measurement of Na+ in the intestine showed that addition of bradykinin to the medium reduced the uptake of Na+ into the tissue and enhanced the efflux of Na+ from the intestine to the medium. Glucose- or valine-evoked transmural potential difference in jejunum segment was elevated by the addition of kallidin to the serosal side, but the transepithelial resistance was not altered. Thus, we suggest that Na+ transport in the small intestine is stimulated by the action of kinins on the serosal side of the intestine, and this acceleration of Na+-flux seems to be accompanied with the enhancement of amino acid and glucose transport.View full abstractDownload PDF (868K) -
YOSHIAKI KAWASHIMA, HIDEO TAKENAKA, HISAKAZU SUNADA, AKINOBU OTSUKA1982 Volume 30 Issue 1 Pages 280-287
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSComputer simulation of agglomeration of mono-sized circles on a two-dimensional plane was undertaken by a random addition model to investigate the mechanism of agglomeration of dispersed particles in a liquid suspension. Under centripetal force, a new circle approached a circle placed on the origin from a random direction. Two types of agglomerations, i.e. closely and loosely packed agglomerations, were simulated by using different process of adhesion of the circles. For the closely packed agglomeration, the internal packing structure was independent of the probability coefficient of adhesion (Pr), but the agglomeration rate was Pr dependent. The packing structure and the agglomeration rate of loosely packed agglomeration were determined by the probability coefficient of adhesion (Pa). Heterogeneous agglomeration was also simulated by defining two types of circles, e.g. A and B, with different adhesion properties, which determined the internal composition and the structure of the agglomerate. By introducing the probability coefficient of collision (Pc), a practical agglomeration process in a batch system in which the residual numbers of particles decrease as the agglomeration proceeds could be described. A layering agglomeration could be visualized by defining Pc as n1/n10. Population balance for this agglomeration led the rate equation expressed by equation (3) in the text. The agglomeration rates of loosely and closely packed agglomerations were determined in terms of Pa and Pr, respectively. The rate of heterogeneous agglomeration was less dependent upon Pa than the others. The internal packing structure of agglomerates strongly depended on Pa ; when Pa increased, the porosity of the agglomerate increased and the average coordination number decreased. The porosity could be correlated qualitatively with the coordination number.View full abstractDownload PDF (867K) -
MASAOKI MIYAHARA, TOMOO TAKAHASHI1982 Volume 30 Issue 1 Pages 288-295
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSolubilization of the slightly soluble drug 3-benzimidoyl-2-hydroxy-1, 4-naphthoquinone was studied by the solubility method using sodium benzoate and several phenol derivatives as solubilizing agents. Their solubilizing mechanism is believed to involve the formation of soluble complexes between drugs and solubilizing agents. Solubility curves observed in cases where complexes of high order were formed at the same time were analyzed by using the nonlinear optimization technique, i.e., the Gauss-Newton method and the conjugate gradient method. Further study is needed to check the accuracy of the estimated parameters.View full abstractDownload PDF (801K) -
YUKIHISA KURONO, HIDETO YAMADA, KEN IKEDA1982 Volume 30 Issue 1 Pages 296-301
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo distinguish the reactive site on human serum albumin (HSA) towards aspirin derivatives from that towards p-nitrophenyl acetate (NPA), the effect of the acetylation of HSA by aspirin and also the effect of several drugs on the reaction rates of substituted aspirins and NPA with HSA were investigated in pH 7.4 phosphate buffer at 25°C. The substituted aspirins examined were 5-nitroaspirin and 3, 5-dinitroaspirin. The acetylation by aspirin affected the reaction rate with 5-nitroaspirin but not that with NPA. The inhibition patterns of the reactions with the aspirins caused by clofibric acid, flufenamic acid and phenylbutazone were different from those with NPA. The complex formation between 5-nitroaspirin and the reactive site of HSA decreased the fluorescence intensity due to the only tryptophan residue (Trp-214) of HSA. These results indicate that the reactive site towards the aspirins (near Trp-214) is different from that towards NPA which was found previously to be near Tyr-411. From the pH profiles of the kinetic parameters for the reaction of 5-nitroaspirin with HSA, the pKa value of the catalytic group constituting the reactive site towards the aspirins was estimated as about 9.5.View full abstractDownload PDF (682K) -
C.O. OKAFOR, M.L. STEENBERG, J.P. BUCKLEY1982 Volume 30 Issue 1 Pages 302-318
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAcid-catalyzed condensation of 2-amino-3-mercapto-6-methylpyridine and 3-amino-pyridine-2 [1H]-thiones with 4-chloropyrimidines having free 5-carbon centers gave N-(3-mercapto-2-pyridyl)-6-pyrimidinylamines and N-(2-thioxo-3-pyridyl)-6-pyrimidinyl-amines, which we have described as open 1, 3, 9-triaza- and 1, 3, 6-triaza-phenothiazines, respectively. A newly developed method of reducing nitro groups was used for preparing the aminopyridine precursors. Eight new and five related compounds including an open 1, 9-diazaphenoxazine were tested in rats and mice and found to display central nervous system (CNS)-depressant activities. The most active compound in the series is N-(6-chloro-2 [1H]-thioxo-3-pyridyl)-2, 4-diamino-6-pyrimidinylamine, an open 1, 3, 6-triaza-phenothiazine derivative. Structure-activity correlations are discussed on the basis of the biological data.View full abstractDownload PDF (1695K) -
Effect of Manufacturing Procedures on the Dissolution and Human Bioavailability of DiphenylhydantoinSHIGERU YAKOU, YAEKO YAJIMA, TAKASHI SONOBE, MASAYASU SUGIHARA, YUKIO ...1982 Volume 30 Issue 1 Pages 319-325
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution characteristics of commercial diphenylhydantoin (DPH) crystals, freeze-dried DPH, 20% simple blend DPH powder, and 20% solvent deposition DPH powder were determined by the use of a USP dissolution test apparatus in pH 1.2 and pH 7.5 test media. The solvent deposition method was found to give DPH with the fastest dissolution rate probably due to improvement in the wettability of the crystals as well as decrease in the particle size. Content uniformity was assessed and accelerated testing of the preparations was also performed to explore optimum formulations. No conversion of the crystal form of DPH or freeze-dried DPH was detected through powder X-ray diffractometry and IR spectrometry under the accelerated storage conditions. Based on the results of the above in vitro studies, 20% DPH solvent deposition powder and the DPH crystals (as a reference) were selected for a bioavailability study in humans. A cross over study in 6 healthy male volunteers revealed the existence of a critical particle size for satisfactory bioavailability. Other factors, such as the use of diluents, also substantially affect the bioavailability of a DPH preparation, even though the crystals used to prepare the finished product were all from the same batch. These results have important implications for manufacturing procedures for DPH preparations.View full abstractDownload PDF (774K) -
HITOSHI YAMAGUCHI, FUMIYOSHI ISHIKAWA1982 Volume 30 Issue 1 Pages 326-332
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis and sodium borohydride reduction of 4-chloro-(1) and 4-unsubstituted-(3) 5, 6, 7, 8-tetrahydro [1] benzothieno [2, 3-d] pyrimidines, substituted with various groups, such as chloro, hydrogen, methyl, phenyl, amino, ethoxy, methylthio, methylsulfinyl and mesyl, at position 2, are described. In the reduction of 1, the 2-chloro and 2-methyl-sulfinyl derivatives only gave the corresponding 3, 4-dihydro derivatives. The compounds 3, except for the 2-phenyl, 2-amino and 2-ethoxy derivatives, were reduced to give the corresponding 3, 4-dihydro derivatives. The reduction was promoted by the presence of an electron withdrawing group at position 2. A 2-or 4-mesyl group was eliminated in the course of the 3, 4-dihydrogenation.View full abstractDownload PDF (822K) -
HITOSHI UNO, MIKIO KUROKAWA1982 Volume 30 Issue 1 Pages 333-335
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHydrogenation of 3-sulfamoylmethyl-1, 2-benzisoxazole (1) gave ω-sulfamoyl-2-hydroxyacetophenone (3) and its imide (2). Treatment of 3 with acid afforded a new route to 1, 2-benzoxathiin-4 (3H)-one-2, 2-dioxide (5). The oxime of 3 (4) was recyclized to provide 1, 2-benzisoxazole derivatives by treatment with acid or base. On pyrolysis 4 gave benzoxazole derivatives.View full abstractDownload PDF (445K) -
KATSUMI TABEI, ETSUKO KAWASHIMA, TOYOZO TAKADA, TETSUZO KATO1982 Volume 30 Issue 1 Pages 336-340
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSO-Acetoacetylbenzamide oxime derivatives (2) were prepared from benzamide oxime derivatives (1) and diketene at low temperature in almost quantitative yields. Cyclization of 2 in the presence of a strong base proceeded with elimination of acetone to afford 3-aryl-1, 2, 4-oxadiazolin-5-one derivatives (4) in 77-95% yields. However, in the cases of the o-, m-, and p-nitrobenzamide oxime derivatives (2f-h), the reaction proceeded with dehydration even in the presence of a strong base to afford 5-acetonyl-3-aryl-1, 2, 4-oxadiazole derivatives (3f-h) in moderate yields. Possible mechanisms of these cyclization are discussed.View full abstractDownload PDF (560K) -
HANDONG SUN, JINHUA CHAO, ZHONGWEN LIN, TERUYOSHI MARUNAKA, YOSHINORI ...1982 Volume 30 Issue 1 Pages 341-343
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new diterpenoid, rubescensin C, was isolated from the leaves of Rabdosia rubescens (HEMSL.) HARA (Labiatae) and its structure was established from spectral and chemical evidence.View full abstractDownload PDF (412K) -
HARUAKI YAJIMA, YOSHIHARU MINAMITAKE, SUSUMU FUNAKOSHI, ITSUKO KATAYAM ...1982 Volume 30 Issue 1 Pages 344-348
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn undecapeptide amide, H-Pyr-Ala-Asp-Pro-Lys-Thr-Phe-Tyr-Gly-Leu-Met-NH2, corresponding to the entire amino acid sequence of an amphibian peptide, [Lys5, Thr6]-physalaemin, was synthesized using the thioanisole-mediated trifluoromethanesulfonic acid deprotection procedure. The synthetic peptide was as active as the natural peptide, in terms of the contractility in guinea pig ileum, and its potency relative to that of synthetic substance P was 0.467.View full abstractDownload PDF (637K) -
KENICHI AKAJI, NOBUTAKA FUJII, HARUAKI YAJIMA, PEARSON DAVID1982 Volume 30 Issue 1 Pages 349-353
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUrotensin II, a somatostatin-like fish hormone, was synthesized in a conventional manner using thioanisole-mediated deprotection with trifluoromethanesulfonic acid. The synthetic peptide was indistinguishable from the natural peptide in terms of both biological activity and chromatographic behavior.View full abstractDownload PDF (734K) -
TETSUO MISAKI, KAZUHIKO SAGARA, MITSUHARU OJIMA, SADAO KAKIZAWA, TOSHI ...1982 Volume 30 Issue 1 Pages 354-357
Published: January 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new, simple method using ion-pair high-performance liquid chromatography was developed for simultaneous determination of berberine, palmatine and coptisine in Coptidis Rhizoma, Phellodendri Cortex and oriental pharmaceutical preparations containing them. A reversed-phase system of ODS-silica gel with a mixture of sodium lauryl sulfate, 0.1N tartaric acid, methanol and acetonitrile (0.5 : 49.5 : 10 : 40) as the mobile phase was used. The three components extracted with the mobile phase could be completely separated within 15 min. The detection limits for the three components were 15 ng at a signal-to-noise ratio of 5 : 1. The results obtained with an ultraviolet detector were in good accord with those obtained with a fluorescence detector.View full abstractDownload PDF (476K)