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Volume 25, Issue 7
Displaying 1-49 of 49 articles from this issue
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JAGDISH PRASAD SHARMA, VIJAI KRISHNA SHANKER SHUKLA, AWADESH KUMAR DUB ...1977 Volume 25 Issue 7 Pages 1493-1496
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA micromethod for determination of pyrrole derivatives using bromine monochloride in acetic acid as the reagent is described. The results obtained show the maximum error of 1.06% on the average.View full abstractDownload PDF (487K) -
KOZO OKADA, MASAYUKI KAWASE1977 Volume 25 Issue 7 Pages 1497-1508
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to establish a simple and rapid method for the differentiation of α- and γ-glutamyl linkages, mass spectra of a series of α- and γ-glutamyl oligopeptides including di-, tri-, and tetrapeptides were examined and the following results were obtained. 1) Generally the spectra of the α- and γ-isomers were distinguishable in several fragment peaks ; particularly, ions c and h arising from the cleavage of glutamyl Cα-CO bond (Chart 2) are characteristic to the α-isomers, while ions e and g due to the ring formation of glutamyl chain (Chart 3) appeared intensely in the γ-isomers. The peak intensity ratios of these ions, c/g and h/e, which were large for the α- and small for the γ-isomers, were especially useful for the assignment of the glutamyl linkages. 2) As a result the whole structures of the α- and γ-glutamyl peptides (up to around tetrapeptide) were easily determined from the mass spectra of their Z or Dec derivatives. 3) All of the four structural isomers of glutamyllysine were easily distinguished from their mass spectra. 4) The method presented here was successfully applied to determine the full structures of some natural glutamyl peptides such as glutathione and cross-linking peptides found in certain peptidoglycans and proteins.View full abstractDownload PDF (1066K) -
YASUHIRO YAMANE, HIDEKI FUKINO, MASAYOSHI IMAGAWA1977 Volume 25 Issue 7 Pages 1509-1518
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMale rats were given mercuric chloride (0.018 mmol/kg/day) by subcutaneous injection and zinc acetate (3.0 mmol/kg/day) by oral administration. Mercury and zinc were administered at the same time, once every 24 hr for 5 days. Only 1 of 10 rats given mercury alone survived for 3 days, and this one rat died on the 4th day. In the group given mercury and zinc at the same time, all the 10 animals were alive on the 5th day, indicating the marked effect of zinc in suppressing the toxicity of mercury. Based on such a marked effect of zinc, examinations were made to see whether biosynthesis of metallothionein would occur in the presence of zinc or mercury by the incorporation of 14C-cysteine into the metallothionein fraction. High rate of incorporation of radioactivity into the metallothionein in the rat liver was observed by the administration of zinc but the incorporation was not so marked by the administration of mercury. This fact suggested that the metallothionein induced by zinc might have some effect on lowering of mercury toxicity and then, distribution of mercury and zinc in the soluble fraction was examined. It was found that, in the liver, mercury bound in larger amount to high molecular fraction during single administration of mercury transited to the metallothionein fraction when zinc was administered concurrently. The amount of mercury bound as Hg-thionein in the kidney after the concurrent administration of mercury and zinc is about 4 times that after single administration of mercury.View full abstractDownload PDF (1106K) -
YOSHINORI TOMINAGA, HIROSHI FUJITO, KAZUMICHI MIZUYAMA, YOSHIRO MATSUD ...1977 Volume 25 Issue 7 Pages 1519-1527
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 1-[2, 2-bis (methylthio) vinyl] pyridinium iodide derivatives (1a-k) with active methylene compounds in the presence of a base in ethanol, dimethylformamide, or dimethyl sulfoxide gave pyridinium allylide, indolizine, and N-[2, 2-bis (methylthio) -vinyl]-N-(6, 6-disubstituted 1, 3, 5-hexatrienyl) amine derivatives.View full abstractDownload PDF (952K) -
YOSHINORI TOMINAGA, YOSHINORI MIYAKE, HIROSHI FUJITO, KEIJI KURATA, HI ...1977 Volume 25 Issue 7 Pages 1528-1533
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of the pyridinium N-ylides with ketenethioacetals in the presence of triethylamine or potassium carbonate as a base in ethanol or dimethylformamide gave the pyridinium N-allylides which were readily cyclized to afford the indolizine derivatives.View full abstractDownload PDF (745K) -
NOBUYOSHI KANENIWA, AKIKO IKEKAWA1977 Volume 25 Issue 7 Pages 1534-1546
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPolyvinylpyrrolidone (PVP) was ball-milled in nitrogen in the presence of chloranil, vitamin K3, acridine, phenothiazine, p-hydroquinone, barbituric acid, white alundum, silica sands, zinc oxide, sodium chloride, activated charcoal or talc. An induction period of 20-120 hours, at the time when molecular weight of PVP began to decrease, was observed in case of ball-milling PVP in the presence of Vitamin K3, acridine, phenothiazine, zinc oxide or talc. The induction period was longer than 200 hours in the presence of chloranil or the granules of activated charcoal. The induction period decreased by the presence of oxygen or the small quantity of the vapor of distilled water or the aqueous solution of hydrogen peroxide in the ball-milling atmosphere. The electron spin resonance (ESR) spectra of the mixtures of PVP and the additive showed that interaction was caused between them by ball-milling. When a large induction period was observed, the intensity of the signal in the ESR spectra increased slightly at the first stage of ball-milling and remarkably by ball-milling after the lapse of the induction period. The scanning electron microscopic photographs of the ball-milled mixtures suggested that the particles of the additive filled in the pores on the surface of PVP and got into the particles of PVP gradually by ball-milling. The molecular weight and the particle size of PVP seemed to begin to decrease after the particles of the additive filled in the pore thoroughly by ball-milling, when a long induction period was observed.View full abstractDownload PDF (2036K) -
HIROSHI KOBAYASHI, TSOCHIN PENG, RURIKO KAWAMURA, SHOZO MURANISHI, HIT ...1977 Volume 25 Issue 7 Pages 1547-1554
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe mechanism of the absorption inhibitory effect of surfactants on the intramuscular absorption of drugs was investigated. The following observations were demonstrated. 1) All surfactants used in this study whether nonionic or ionic caused solubilization of muscle protein. A good correlation between the solubilization of muscle protein and the absorption inhibitory effect was also found except in the case of the nonionic surfactant HCO-120. 2) The effect of hyaluronidase in the absence or presence of various concentrations of polysorbate 80 on the intramuscular absorption of drugs of different molecular weight was examined. The coexistence of hyaluronidase and polysorbate 80 greatly affected the absorption of drugs. This was depending upon the molecular size of diffused drug and the concentration of surfactant. It was found that increasing the concentrations of polysorbate 80 in the presence of hyaluronidase was accompanied by an inhibition in the absorption of isonicotinamide and abolishment of the accelerating effect of hyaluronidase on the absorption of 14C-sucrose, but it could not show any effect on the absorption of 14C-inulin. 3) The permeability coefficient of gelatin-sodium chondroitin sulfate mixed membrane in the presence of polysorbate 80 was decreased significantly. From these results, it can be concluded that the surfactants interacted with proteins and mucopolysaccharides which are the main components of connective tissue, consequently the intramuscular absorption of drugs was extremely inhibited.View full abstractDownload PDF (868K) -
HIROSHI SAKAGUCHI, HIROSHI ANZAI, TADAO FUJITA, TAKEICHI SAKAGUCHI1977 Volume 25 Issue 7 Pages 1555-1558
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCopper (II), cobalt (II), nickel (II), and zinc (II) complexes of 2-hydrazino-4-hydroxy-6-methylpyrimidine were synthesized, and their infrared (IR) and nuclear magnetic resonance (NMR) spectra were examined. In the IR spectra of the complexes, the amide-I (carbonyl) bands were present and it was assumed that the ligand molecules were coordinated in the keto form of the isocytosine ring. The low frequency shift of the NH2 stretching bands by about 40-45 cm-1 on combining with Cu and Co indicated the formation of a metal-nitrogen bond. Preferential broadening of methine proton to methyl proton in the NMR spectra of the complexes of 2-hydrazino-4-hydroxy-6-methylpyrimidine can be explained by the binding of Co (II), Cu (II), and Ni (II) to N (3) site of the isocytosine ring. An ESR spectrum of the copper (II) complex would suggest the presence of copper (II) ion in a square-pyramidal conformation.View full abstractDownload PDF (523K) -
KAZUO MURATO, TAKAYUKI SHIOIRI, SHUNICHI YAMADA1977 Volume 25 Issue 7 Pages 1559-1565
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(3S)-tert-Butyl 2-benzyloxycarbonyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carbamate (III), prepared by the modified Curtius reaction of (3S)-2-benzyloxycarbonyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid (II) with diphenyl phosphorazidate (DPPA) and triethylamine in tert-butyl alcohol, afforded 2-ethyloxycarbonylaminomethyl-3-(2-tert-butyloxy-carbonylamino) ethylindole (Va) by sodium borohydride reduction in ethanol, while reduction in 2-propanol gave the corresponding 2-propyl derivative (Vb) and the compound (VI) containing a novel diazocinoindole skeleton. The mechanism of the reductive cleavage was discussed. Tetrahydropyrrole analog (X) of III and 2-acetyl analog of III afforded the similar ring-cleavage products (XI and XV) by sodium borohydride reduction.View full abstractDownload PDF (785K) -
HIROSHI KIWADA, MASAHIRO HAYASHI, TOHRU FUWA, SHOJI AWAZU, MANABU HANA ...1977 Volume 25 Issue 7 Pages 1566-1573
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe fate of 8-hydroxyquinoline (Oxine) (OX) in rats, which is the parent compound of iodochlorhydroxyquin (chinoform, 5-chloro-8-hydroxy-7-iodoquinoline) (I) suspected to cause SMON, was investigated. Although both OX and I are metabolized to glucuronide and sulfate, the differences obtained from the excretion data are as follows : 1) After the intravenous administration of OX, glucuronide was more excreted (about 65% of dose) than sulfate (about 25% of dose) in urine in contrast to the case of I. 2) In bile, only 10% as glucuronide was excreted. The difference from I was considered due to the difference of molecular weight caused by the halogen substitution. 3) Both OX glucuro nide and sulfate were stable in the body, and it was excreted as the administered form without exchanging to the another form after the intravenous administration of each conjugate. Accordingly the fate of these compounds in the body was shown to be well influenced by the halogenation. Furthermore, the blood concentration of free and conjugated OX, which was determined with synthesized 14C-OX, was analyzed by the application of numerical deconvolution technique to the precursor-successor relationship between OX and each conjugate. Consequently, the usefulness of the technique was demonstrated and some pharmacokinetic features for OX were obtained.View full abstractDownload PDF (799K) -
RENSUKE GOTO, MASAKATSU TEZUKA, OSAMU TAMEMASA1977 Volume 25 Issue 7 Pages 1574-1581
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFor the development of amino acid derivatives as a new pancreas-scanning agent, comparative experiments were made on the in vivo incorporation of 18 kinds of 14C-labeled L-amino acid, and of D- and DL-forms of four selected radioactive amino acids into the trichloroacetic acid (TCA)-soluble and protein fractions of the pancreas and liver of mice. Among the L-forms tested, tryptophan, valine, methionine, and leucine, in this order of decreasing incorporation, showed a relatively high incorporation into the pancreas 30 min after intravenous injection. Pancreas/liver ratio of the radioactivity of methionine, valine, and leucine determined 15, 30, and 60 min after injection were 6 to 10. Although all of the amino acids were not predominantly high in pancreas/liver ratio compared with selenomethionine-75Se, the three amino acids seem a possible mother compound for introducing γ-emitters as a pancreas-scanning agent. In the TCA-soluble fraction of the pancreas, radioactivity of DL- or D-amino acids tested was higher than that of the corresponding L-amino acid. In particular, the almost whole radioactivity of D-leucine was found in the TCA-soluble fraction, and the activity due to D-leucine-14C itself. The incorporation of D-leucine into the pancreas was much the same as L-leucine. Based on these results, γ-radiating derivatives of amino acids might be useful as a new pancreas-scanning agent.View full abstractDownload PDF (866K) -
AKIRA TAKAMIZAWA, SAICHI MATSUMOTO, TSUYOSHI IWATA, SHOJI SAKAI, ITSUO ...1977 Volume 25 Issue 7 Pages 1582-1590
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNew cyclophosphamide derivatives having the 1, 3, 4, 2-oxadiazaphosphorinane and related heterocyclic systems were prepared by the ozonolysis reactions of O-(2-propenyl)-and O-(3-butenyl)-N, N-bis(2-chloroethyl) phosphoramidoyl hydrazides and their derivatives. The newly synthesized heterocyclic systems were dihydro-6H-1, 3, 4, 2-oxadiazaphos-phorine-2-oxide, 4-acetyl-5-hydroxy-1, 3, 4, 2-oxadiazaphosphorinane-2-oxide, 4-acetyl-5-hydroxyhexahydro-2H-1, 3, 4, 2-oxadiazaphosphepine-2-oxide and perhydro-1, 3, 4-oxadiazolo [3, 2-c]-1, 3, 2-oxazaphosphorine-1-oxide. Comparative studies of the in vivo antileukemic activity revealed that these cyclophosphamide derivatives were ineffective in promoting the antitumor action.View full abstractDownload PDF (1114K) -
MASANAO TERASHIMA, KOICHI SEKI, KOICHI KOYAMA, YUICHI KANAOKA1977 Volume 25 Issue 7 Pages 1591-1595
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotochemical reactions of N-methylpyridylphthalimides (VII-IX) were investigated. Although irradiation of VII in an acetone solution gave only the dihydro product, 3-hydroxy-2-(3-methyl-2-pyridyl) phthalimidine (X), VIII afforded the expected cyclized product, 10b, 11-dihydro-10b-hydroxy-6H-pyrido [4', 3' : 4, 5] pyrrolo [2, 1-a] isoindol-6-one (XII) and dihydro product, 3-hydroxy-2-(4-methyl-3-pyridyl) phthalimidine (XI). Under similar conditions, the cyclized product, 10b, 11-dihydro-10b-hydroxy-6H-pyrido [3', 4' : 4, 5]-pyrrolo [2, 1-a] isoindol-6-one (XIII) was obtained from the photolysis of IX and none of the reduced product was isolated.View full abstractDownload PDF (606K) -
ATSUSHI SUGII, NAOTAKE OGAWA, TAKASHI OCHIAI1977 Volume 25 Issue 7 Pages 1596-1600
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo macroreticular resins containing β-diketone groups were prepared and their adsorptivity for nine metal ions was investigated by batch operation. Although these resins were highly selective for Fe (III) in acidic region (pH 1-4), no significant affinity was observed for Cd (II), Co (II), Cu (II), Mg (II), Mn (II), Ni (II), Zn (II), and U (VI). The β-diketone resin prepared from styrene-divinylbenzene copolymer and diketene was applicable to the separation of 59Fe and 60Co by a column operation.View full abstractDownload PDF (528K) -
AKIRA MIZUTANI, TAKAHARU MIZUTANI, IKUKATSU SUZUKI, POFENG KUO1977 Volume 25 Issue 7 Pages 1601-1606
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hypocalcemic substance isolated from bovine parotid gland and the fractions obtained in process of purification were examined for increasing antibody-producing cells (PFC activity) in the spleen of ICR mice by the method of Jerne and Nordin, and for lymphocyte-increasing action in mice. The intraperitoneal injection of the final purified sample in a dose of 10 μg/mouse produced 79.20±15.73 of PFC number per 106 cells in the spleen of neonatal mice. The difference between the mean of PFC number in the test group and that in the control group was significant at 5% level of significance. The final purified product was increased in PFC activity by 10 times that of the acetone-dried powder (starting material). A tendency to the increase in PFC activity and in lymphocytes increasing activity was found in proportion to the increase in hypocalcemic activity. Therefore, it was found that there was an action of promoting immune competence in the hypocalcemic substance. Further, the immunoactivities of parotid hypocalcemic substance were discussed in comparison with the thymic hypocalcemic substances.View full abstractDownload PDF (857K) -
TOSHIAKI MORIMOTO, MINORU SEKIYA1977 Volume 25 Issue 7 Pages 1607-1609
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new one step chloropyrimidinone ring-closure of the conjugated -N=C-N=CH-system of α-arylmethyleneamino-substituted derivatives of pyridine, quinoline, and isoquinoline has been achieved by allowing them to react with trichloroacetic anhydride.View full abstractDownload PDF (461K) -
YOSHINOBU FUKUMORI, JUTARO OKADA1977 Volume 25 Issue 7 Pages 1610-1635
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe theory of the limiting equilibrium states specified by the Mohr criterion was developed for the axially symmetrical problem in regard to tabletting. The unique solution of the equilibrium equations could be obtained when the stress field and the displacement field, which was calculated by using the stress-strain relations and the displacement-strain relations, satisfied the following boundary conditions : (1) the stress on the die wall satisfies the wall yield condition and the active pressure is applied to the die wall ; (2) the powder does not slide on the punches ; (3) the displacement at the die wall is produced only in the direction parallel to die wall. The above relations were derived on the base of the incremental theory and the theory of the velocity field in soil mechanics. The mechanical properties which were required for the numerical calculations on the computors were the yield locus, the wall yield locus and the stress-strain relation in the one-dimensional compression, which were obtained experimentally with the potassium chloride powder. The results of calculations showed that there appeared the region where the pressure was higher than in the neighbourhood and the region where the pressure was lower when the upper punch pressure changed from zero to 2 kg/cm2.View full abstractDownload PDF (1869K) -
YASUO INUBUSHI, YOSHIKUNI ITO, YUKIO MASAKI, TOSHIRO IBUKA1977 Volume 25 Issue 7 Pages 1636-1644
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBisbenzylisoquinoline alkaloids, trilobine (2 : R-H) possessing a dibenzo-p-dioxin nucleus and obaberine (3) were synthesized. dl-O-Benzyl-8-bromo-N-norarmepavine (10 : R=H) synthesized through an established route was resolved and N-benzoylation of the resolved free base, followed by condensation with the amine (12) gave the diphenyl ether (13a). Debenzylation of 13a, followed by condensation with the compound (14) gave the ester (15a) which was cyclized to the cycloamide (17) via the phenethylammonium trifluoroacetate (16). Bischler-Napieralski reaction of the amide (17) and reduction of the imine (18), followed by N-methylation afforded the compound (19b) and (5) in a 2 : 5 ratio. Successive treatments of the compound (19b) with LiAlH4-AlCl3, hydrogen on Pd-C catalyst and HCHO-NaBH4 afforded obaberine (3). On the other hand, the N-benzyl base (19c) from the compound (5) was demethylated to give the demethyl base (20) which was heated in a saturated aqueous HBr solution to provide the compound (21). Finally, treatment of the compound (21) with CH2N2, followed by hydrogenolysis on Pd-C catalyst gave trilobine (2 : R=H).View full abstractDownload PDF (1132K) -
TOKIO SAITO, TETSUO HIRAOKA1977 Volume 25 Issue 7 Pages 1645-1650
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermolysis of phosphorus ylides (III and XIV), obtained by the reactions of the iminophosphoranes (II and XIII) with dimethyl acetylenedicarboxylate, afforded the imino derivatives (IV and XV) with elimination of triphenylphosphine. These imino compounds, IV and XV were methoxylated with lithium methoxide to yield the α-methoxy-amino-acid (X) and 7α-methoxy-cephalosporin (XVI), respectively.View full abstractDownload PDF (744K) -
HARUO SAIKACHI, TOKUJIRO KITAGAWA1977 Volume 25 Issue 7 Pages 1651-1657
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-Substituted 2-furoyl azides (7a, 7b and 7c), 5-substituted 2-thenoyl azides (7d, 7e and 7f), 2-, 3- and 4-pyridinemonocarbonyl azides (7j, 7k and 7l) and p-substituted benzoyl azides (7g, 7h and 7i) were prepared from the corresponding carboxylic acids with DPPA (4) in one step and in good yields, respectively. It was found through the kinetic studies that an electron-withdrowing group substituted at 5-position (furan and thiophene ring) or p-position (benzene ring) decreases the rate of the reaction, and reversely, an electron-donating substituted at 5- or p-position increases it. In addition, it looks to be reasonable that the most probable pathway is to form the above acyl azides via the activated six-membered cyclic complex (9) as an intermediacy and then to proceed in the concerted reaction, based on the activation energies (ΔE*) and entropies (ΔS*) obtained.View full abstractDownload PDF (758K) -
SABURO NAKANO, TOMOHIKO YOSHIDA, HIROKAZU TANIGUCHI, NORIKO SUZUKI1977 Volume 25 Issue 7 Pages 1658-1664
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwenty-nine derivative of quinoline-2-thiol were synthesized from thiourea and 2-bromo (or 2-chloro) quinoline derivatives. The limit of identification for metal ions with these reagents was examined by a spot test. These reagents gave a precipitate with the following metal ions : Cu+, Cu2+, Pd2+, Ag+, Pt4+, Au3+, Hg2+2, Hg2+, and Bi3+. The effect of substituted groups on molecular extinction coefficient and wavelength of maximum absorption of reagents, of palladium (II) complexes, and of copper (I) complexes was studied. In these reagents, 4-phenyl-7-methoxyquinoline-2-thiol and 4-methyl-8-ethoxy-quinoline-2-thiol were the most sensitive reagents for palladium (II) and copper (I) in an acetic acid solution. Extraction of palladium (II) complexes with an immiscible organic solvent was also examined.View full abstractDownload PDF (728K) -
TETSURO NAGASAWA, HIKOKICHI OURA, SUSUMU HIAI, KEIJI NISHINAGA1977 Volume 25 Issue 7 Pages 1665-1670
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdministration of the extract from the roots of Panax ginseng C.A. MEYER increased the incorporation rate of labeled precursor into rat renal nuclear RNA, this stimulating effect was dose dependent, and the maximum activity was observed at 8 hr after the treatment. The sequential cytoplasmic RNA synthesis was stimulated maximally at 10 hr after the administration. The stimulating effect of the ginseng extract on RNA synthesis resulted in an increased incorporation of labeled leucine into rat renal protein and the maximum activity was observed at 12 hr after the intraperitoneal administration.View full abstractDownload PDF (713K) -
HIDEAKI UMEYAMA, SETSUKO NAKAGAWA1977 Volume 25 Issue 7 Pages 1671-1677
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the solvolysis of aspirin and acyl-α-chymotrypsin, the significant fact is the rate acceleration by the addition of alcohol in water solution. The authors reported that the rate acceleration of the hydrolysis occurs as the content of alcohol increases, since a water of the monomer state reacts with the ester part of aspirin or acyl-α-chymotrypsin. The mechanism was clarified by using nonempirical molecular orbital method. The proton removal energy for methanol corresponds to that for 1.4 waters. The difference of the proton removal energy between CH3OH and H2O is attributed to the electrostatic interaction term. On the other hand the main contributor for the difference between CH3OH and (H2O)2 is the polarization interaction term. Moreover the difference between H2O and (H2O)2 is due to the electrostatic interaction term. For the interaction energies between ester and hydroxyl ion and between ester and water, the charge transfer interaction term and the electrostatic interaction term, respectively, were significant.View full abstractDownload PDF (754K) -
MINORU MACHIDA, MIKIKO I. MACHIDA, TAKAMITSU SEKINE, YUICHI KANAOKA1977 Volume 25 Issue 7 Pages 1678-1684
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-(7-Dimethylamino-4-methyl-3-coumarinyl) maleimide (DACM) was applied to egg albumin and it was found that approximately 0.6 mol of DACM was incorporated into the protein molecule as revealed by chemical and spectroscopic analyses. DACS as the model compound of the reaction product of DACM with thiols was used for dependency of pH and solvent.View full abstractDownload PDF (790K) -
HIDEAKI UMEYAMA, AKIRA IMAMURA, CHIKAYOSHI NAGATA, SETSUKO NAKAGAWA1977 Volume 25 Issue 7 Pages 1685-1693
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe mechanism of the enzymatic reaction of lactate dehydrogenase was studied from the quantum chemical point of view. The charge relay system composed of aspartate, histidine and lactate of the substrate or pyruvate enol of the inhibitor was assumed. The substrate or the inhibitor played a role as a proton donor like serine in the "charge relay system"of α-chymotrypsin. Moreover arginine 171 for the assumed charge relay system was very significant in order to lower the potential barrier of the proton transfer from the substrate or the inhibitor to histidine 195. Last the significance of the HOMOLUMO interaction between the substrate or the inhibitor and nicotinamide in NAD+was shown.View full abstractDownload PDF (830K) -
TADAO FUJITA, TAKEICHI SAKAGUCHI1977 Volume 25 Issue 7 Pages 1694-1700
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA mixed ligand complex, copper-(adeninato) (diethylenetriamine) monohydrate, was prepared and the coordination site of the compound was suggested from infrared spectroscopic analysis. Assignments of infrared bands of this compound are discussed in some detail. Electron paramagnetic resonance (EPR) spectra of this compound were recorded at room temperature and the EPR spectral line shape and g-values were compared with those of other mixed ligand complexes containing the adenine ligand. It was assumed that the coordination sphere of Cu2+ was a square-based pyramidal and the nitrogen atom N9 of adenine monoanion coordinated with Cu2+.View full abstractDownload PDF (641K) -
TETSUYA KOMORI, TOSHIO KAWASAKI, KAZUHIDE KAMIYA, YOSHIKAZU WADA1977 Volume 25 Issue 7 Pages 1701-1707
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDie Losung der Struktur von 3-Bromo-2-oxo-tetrahydrodiosbulbin-A (5) erfoigte rontgenographisch mit Schweratom-Methode. Die Verfeinerung nach der Block-Diagonal-Least-Squares-Methode konvergierte bei einem R-Wert von 10.6% (fur 1120 independente Reflexe). Die absolute Konfiguration von 5 wurde mit Bijvoet-Methode bestimmt. Die absolute Konfiguration von Tetrahydrodiosbulbin-A, Diosbulbin-A, -B und -C, die auf chemisch physikalischem Wege nicht eindeutig bestimmt werden konnte, wurde daher festgelegt.View full abstractDownload PDF (777K) -
MITSUJI YANAI, SHIGEKO TAKEDA, TAMAO MITSUOKA1977 Volume 25 Issue 7 Pages 1708-1716
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Cyano-3, 6-dichloropyridazine (II) was treated with primary amines in methanol under mild condition (stirring at 0-5°) to give neither the corresponding 3- nor 6-amino derivatives but the corresponding 5-amino derivatives (XVd-m) resulting from nuclear amination. However, when compound II was treated with secondary amines, the corresponding 3- or 6-amino derivatives were obtained.View full abstractDownload PDF (978K) -
YOSHIHIRO NISHIKAWA, KIMIHIRO YOSHIMOTO, MUTSUKO OKADA, TETSURO IKEKAW ...1977 Volume 25 Issue 7 Pages 1717-1724
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAccrding to the procedure of Osipow, sucrose was partially acylated with palmitic, stearic, hydnocarpic, and ricinoleic acids. In the similar manner, the selective esterification of trehalose was performed, using caprylic, lauric, myristic, and stearic acids. The ester compositions of the resulting preparations were preliminarilly analysed by means of thin-layer chromatography and gas chromatography, and the major components contained in them were tentatively assigned to the 6-monoesters of these disaccharides. All the preparations obtained proved to exert considerable antitumor effect against Ehrlich ascites carcinoma in mice by intraperitoneal administration.View full abstractDownload PDF (955K) -
AKIRA KONO, YOSHIKAZU MATSUSHIMA, MASAHARU KOJIMA, TATSUO MAEDA1977 Volume 25 Issue 7 Pages 1725-1731
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCobalt chelate of bleomycin (Co-BLM) was inert to ligand exchange reaction and showed absorption at 450 nm and 580 nm, which indicated cobalt is trivalent. Co-BLM was accumulated in tumor tissue much more than BLM and other BLM metal chelates. In urine of 67Ga-BLM or 111In-BLM injected mice, most of radioactivity was not bound to BLM. On the other hand, all the radioactivity was attributable to BLM bound 57Co in urine of 57Co-BLM injected mice. In tumor tissue homogenate, most of Co-BLM was present in cell nuclei, while BLM, CoCl2 and other BLM metal chelates distributed mainly in supernatant fractions. Co-BLM may bind to deoxyribonucleic acid (DNA) in tumor cell. From these results, we conclude Co-BLM to be superior as a tumor scanning agent than BLM and other BLM metal chelates.View full abstractDownload PDF (854K) -
KAZUO ITO, HITOSHI TANAKA1977 Volume 25 Issue 7 Pages 1732-1739
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-Sulfonylphenethylamines (6-9) have been readily condensed with formaldehyde under mild acidic condition to the corresponding N-sulfonyl-1, 2, 3, 4-tetrahydroisoquinolines (14-17) in excellent yields. Condensation of sulfonamide (10) with formaldehyde under similar condition gave a mixture of two cyclization products (18 and 19). In the case of similar condensation of 3, 4-disubstituted-N-sulfonamides (11 and 12) with formaldehyde, 6, 7-disubstituted products (20 and 21) were obtained alone. Similar reaction of sulfonamides (6, 11 and 12) with aliphatic aldehydes or aromatic aldehydes also afforded the corresponding N-tosyl-1, 2, 3, 4-tetrahydroisoquinolines (22-27). Furthermore, 1-benzyl-N-tosyl-1, 2, 3, 4-tetrahydroisoquinolines (31 and 37) were similarly synthesized from sulfonamide (12 or 13) and phenyl acetaldehyde (30 or 36). Birch reduction of (37) afforded the racemic form (33) of natural N-nororientaline, which was previously isolated by us from the leaves of Erythrina X bidwillii (Leguminosae).View full abstractDownload PDF (947K) -
TSUNEMASA AZUMA, TSUNEO SAITA, KIYOSHI ISONO1977 Volume 25 Issue 7 Pages 1740-1748
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA number of aminoacyl derivatives of nucleoside antibiotics, polyoxins C and L were prepared. Aminoacylation was performed in aqueous dimethylformamide with an equimolar N-carbobenzoxyamino acid p-nitrophenyl ester in the presence of an equimolar triethylamine or N-methylmorpholine. Catalytic hydrogenolysis of the condensation product followed by chromatographic purification afforded the aimed compounds in moderate yields. Antifungal activities were tested with several lines of phytopathogenic fungi, which led to some conclusion upon structure-activity relationship regarding the N terminal amino acid : (1) the α-L-amino group is essential for the activity, (2) the alkyl chain length and especially nature of the ω-substituents affect considerably the activity. Many of the aminoacyl derivatives of polyoxin L retained moderate activity. None of the compounds prepared showed broader antimicrobial spectrum than the natural polyoxins.View full abstractDownload PDF (1089K) -
TAKEHISA KUNIEDA, TOSHINARI TAMURA, TAKEO TAKIZAWA1977 Volume 25 Issue 7 Pages 1749-1755
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNickel carbonyl in tetrahydrofuran reductively converts polyhalomethyl groups into di-(or mono-) halomethyls in high to moderate yields under quite mild conditions. Polyhalides studied here include type 1 telomers, arising from the radical reaction of vinylene carbonate and polyhalomethanes, whose successful reduction to gem-dihalides opens up a new route to aldo-sugars. Tetrahydrofuran is the most effective for the reduction among the solvents examined such as isopropanol, dioxane, tetrahydrothiophene, cyclohexene (-hexane) and benzene, while dimethylformamide gives the entirely different products like the olefines (9, 10) and the carboxylic acids (11, 12). The plausible mechanisms involving radical and carbene intermediates are discussed for the reactions in both solvents.View full abstractDownload PDF (775K) -
YUJI NAKAHARA, TETSUKICHI NIWAGUCHI, HISASHI ISHII1977 Volume 25 Issue 7 Pages 1756-1763
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEpimeric pairs of dihydrolysergic acid diethylamide and dihydroisolysergic acid diethylamide were synthesized by hydrogenation of lysergic acid diethylamide (LSD) and iso LSD. Lysergol was obtained by LAH reduction of methyl lysergate which was prepared by treatment of a solution of lysergic acid in HMPA with diazomethane. From lysergol, lysergine and isolysergine were prepared. Festuclavine, pyroclavine, and costaclavine were synthesized by reduction of agroclavine with metal sodium in butanol and their structures were chemically confirmed. ORD curves of these alkaloids were determined and discussed.View full abstractDownload PDF (962K) -
AKIRA YAGI, KENJI MAKINO, ITSUO NISHIOKA1977 Volume 25 Issue 7 Pages 1764-1770
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhenolic constituents of young subterranean stems of Aloe saponaria HAW. were investigated to give aloesaponol III, -IV, chrysophanol, helminthosporin and 1, 4, 8-trihydroxy-2-methoxy-6-methyl-anthraquinone (isoxanthorin). The structures of aloesaponol III and -IV were established to be 1-oxo-4 (S, equatorial), 8, 9-trihydroxy-6-methyl-1, 2, 3, 4-tetrahydroanthracene and 1-oxo-4 (quasi-equatorial), 8, 9-trihydroxy-2-methoxy (equatorial)-6-methyl-1, 2, 3, 4-tetrahydroanthracene on the basis of chemical and spectral evidences. The application of the extended benzoate chirality rule was attempted to determine the absolute configuration of hydroxyl group in aloesaponol I and -III.View full abstractDownload PDF (843K) -
AKIRA YAGI, KENJI MAKINO, ITSUO NISHIOKA1977 Volume 25 Issue 7 Pages 1771-1776
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhenolic glycosides of young subterranean stems of Aloe saponaria HAW. were examined to afford compound A-F. On the basis of chemical and spectral evidences the structures of compound A (I), B (III), C (IV), D (V), E (VI) and F (VII) were determined to be 3-(1'-hydroxyethyl)-4-methoxy-5-hydroxy-2-naphthoic acid lactone 5-O-β-D-glucopyranoside (I), aloesaponol III 8-O-β-D-glucopyranoside (III), aloesaponol I 6-O-β-D-glucopyranoside (IV), aloesaponol II 6-O-D-glucopyranoside (V), aloenin (VI) and aloesin (VII), respectively.View full abstractDownload PDF (816K) -
MIKIO TAKEDA, MASATOSHI KAWAMORI, KATSUYUKI NOGUCHI, SEIICHI NURIMOTO1977 Volume 25 Issue 7 Pages 1777-1781
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs part of study on the structure-activity relationships of phenylazabicycloalkane analgetics, the title compound (I) has been synthesized. Structure (I) could be regarded as a piperidine analog of 1-phenyl-6-azabicyclo [3. 2. 1] octane (II), a known partial agonist, and also as a conformationally constrained analog of the 3-phenyl-piperidine analygetics (XIX). From the keto ester (III), I was obtained by the sequence of reactions outlined in Chart 2. Neither by the AcOH writhing nor by the hot-plate method, I exhibited appreciable analgetic activity. In contrast, the N-methyl compounds (XIV and XV) showed narcotic antagonist activity, with the former being the more active. Replacement of the N-methyl group of XV by a propyl and an allyl group (XVIIIa, d) resulted in an increase in the antagonist activity. Their activity was about one-tenth that of nalorphine.View full abstractDownload PDF (629K) -
KEIJI SEKIGUCHI, KENICHI SHIROTANI, MOTOKO KANKE1977 Volume 25 Issue 7 Pages 1782-1790
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution rates of sulfanilamide in the solutions of two kinds of carboxymethylcellulose sodium (CMC-Na) in the presence or absence of NaCl were measured by the fixed disk method. At the same time, viscosities of these solutions were determined at various rates of shear with a cone and plate viscometer. In the case of simple CMC-Na solutions, it was found that the dissolution rate of sulfanilamide depends almost only upon the viscosity of the solution, irrespective of the degree of polymerization of CMC-Na. Also, it is supposed that the decrease in the dissolution rate occurs by different mechanisms according to whether the solution belongs to the Newtonian or to the non-Newtonian fluid. On the other hand, additional influences due to the actions by NaCl become more or less evident in the mixed solutions of CMC-Na and NaCl. One of them is the salting-out effect and has a tendency to decrease the dissolution rate, while the second acts to increase the rate through viscosity decrease of the solutions by shrinking CMC-Na molecules.View full abstractDownload PDF (864K) -
MASAYOSHI HORIOKA, TOSINOBU AOYAMA, HIRONOBU KARASAWA1977 Volume 25 Issue 7 Pages 1791-1796
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMechanical measurement of particles in the infusion fluid contained in a polyvinyl chloride (PVC) bag revealed the presence of a large number of particles and principle of these particles was examined. It was thereby confirmed that the majority of particles in the solution contained in a PVC bag are liquid particles of di (2-ethylhexyl) phthalate (DEHP) used as a plasticizer for PVC, and these particles adhere to the inner wall of the bag or float in the solution. When the PVC bag is shaken before sampling the fluid, the liquid particles of DEHP are liberated and dispersed as microparticles which are counted as particles by HIAC automatic counter, but not observed on membrane filter under a microscope. Detecting of such a liquid particle, a considerable difference between the results from a mechanical method and that from a microscopic observation was pointed out.View full abstractDownload PDF (947K) -
TAKEFUMI MOMOSE, SHUJI UCHIDA, MASAHIKO KINOSHITA, TAKESHI IMANISHI1977 Volume 25 Issue 7 Pages 1797-1802
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESScis-Octahydro-7 (1H)-quinolone (III) was synthesized stereoselectively by two different routes, one via intramolecular Michael addition of an amino enone (IV) and the other via catalytic hydrogenation of a bicyclic lactam (V). Detailed examinations of hydrogenation products in the latter was also described.View full abstractDownload PDF (800K) -
ZENICHI HORII, MOTOHIDE TSUJIUCHI, KENICHI KANAI, TAKEFUMI MOMOSE1977 Volume 25 Issue 7 Pages 1803-1808
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of taiwanin E was re-examined with an empirical proton magnetic resonance (1H-NMR) rule for the lactone methylene in aromatized naphthalide lignans, and concluded to be 5 instead of 4 on the basis of their unambiguous synthesis. Related lignans : taiwanin C (3), justicidin D (neojusticin A) (6), E (7), and F (taiwanin E methyl ether) (8) were also synthesized. The 1H-NMR rule was found to be the case also with the lignans synthesized.View full abstractDownload PDF (790K) -
TAKEHISA KUNIEDA, TAKEO TAKIZAWA1977 Volume 25 Issue 7 Pages 1809-1810
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOne-step efficient route to tetraarylbutatrienes was provided by the reaction of 1, 1, 1-trihalo-2, 2-diarylethanes or 1, 1-dibromo-2, 2-diphenylethylene with metallic copper (or cuprous chloride) in dimethylformamide at 20-45°.View full abstractDownload PDF (354K) -
KIYOMI KIKUGAWA, HIDEO SUEHIRO, AKIJI AOKI1977 Volume 25 Issue 7 Pages 1811-1821
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of S-substituted 2-thioadenines (VII) and S, 9-di-substituted 2-thioadenines (VIII) were prepared by direct alkylation of 2-thioadenine (IV). Among the compounds synthesized, 2-cyclopentylthio-9-methyladenine (VIII7), 2-cyclopentylthio-9-cyclopentyl-adenine (VIII20) and 2-[2-(4-benzylpiperazino) ethyl] thio-9-[2-(4-benzylpiperazino) ethyl]-adenine (VIII22) were inhibitory against adenosine 5'-diphosphate induced platelet aggregation but these were less potent than adenosine.View full abstractDownload PDF (1218K) -
HIROSHI YAMANAKA, HIROYUKI ABE, TAKAO SAKAMOTO, HIDETOSHI HIRANUMA, AT ...1977 Volume 25 Issue 7 Pages 1821-1826
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethyl groups at the 4-position of 2, 4-dimethyl-, 2, 4, 6-trimethyl-pyridine, 2, 4-dimethyl-, 2, 4, 6-trimethyl-pyrimidine, 2, 4-dimethylquinoline, and 2, 4-dimethylquinazoline were nitrosated selectively with ethyl nitrite in the presence of alkali amide in liquid ammonia to give the corresponding 4-aldoximes. On heating with phosphoryl chloride, the aldoximes were converted to 4-carbonitriles except 2-methylquinazoline-4-aldoxime which was sublimated with phosphorous pentoxide to afford 4-cyano-2-methylquinazoline. Related to these synthetic experiments, the hydrogen-deuterium exchange reaction of the methyl groups was examined by means of the NMR technique. The observed results did not contradict the direction of nitrosation of the testing compounds.View full abstractDownload PDF (717K) -
KAI CHEONG CHAN, KOK FEF MAK, L.E. TEO1977 Volume 25 Issue 7 Pages 1826-1829
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPresented here are the results of further screening of Malaysian plants consisting of 148 species from 61 families, for the presence of alkaloids, saponins, steroids and triterpenes.View full abstractDownload PDF (484K) -
ISAMU MURAKOSHI, AKIHIRO SANDA, JOJU HAGINIWA1977 Volume 25 Issue 7 Pages 1829-1832
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSL-Serine O-sulphate (L-SOS) lyase, an enzyme capable of degrading L-SOS to pyruvate, ammonia and sulfuric acid, was newly found in extracts from higher plants. The optimum pH for the L-SOS lyase in higher plants differ from that for the enzyme (s) in animals and micro-organisms in the same buffer. The distribution and some properties of the L-SOS lyase in higher plants are described.View full abstractDownload PDF (499K) -
HIDEO OISHI, YOICHI USHIO, KAZUMI NARAHARA, MITSUNORI TAKEHARA, TOSHIO ...1977 Volume 25 Issue 7 Pages 1833-1836
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCorrections for misprints and erroneous descriptions are given with some complementary explanations.View full abstractDownload PDF (493K) -
TSUTOMU KAMEYAMA, TOSHITAKA NABESHIMA, MAKOTO UKAI1977 Volume 25 Issue 7 Pages 1837-1839
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn investigation of the pharmacological mechanism of the Straub tail reaction (STR) was made of the intracerebral (i.c.) injection of morphine. In addition, the effects of central muscle relaxants on the STR were examined. The STR was elicited by i.c. injection of morphine. Meprobamate, haloperidol, 1, 3-diphenyl-5-(2-dimethylaminopropionamide)-pyrazole [difenamizole] and β-(p-chlorophenyl)-γ-aminobutyric acid [baclofen] apparently decreased the STR by systemic administration. In mice injected i.c. with difenamizole or baclofen, moreover, the STR was noticeably inhibited. Especially, baclofen decreased the STR in the approximate one-thousandth of the dose by systemic administration. Thus it appears that the central nervous system may have a profound significance for the manifestation of the STR due to morphine in mice.View full abstractDownload PDF (455K) -
SHIKIFUMI KITAZAWA, IKUO JOHNO, HAJIME ITO, FUMIE MORITSUJI, HIDEO TAK ...1977 Volume 25 Issue 7 Pages 1839-1841
Published: July 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSulfanilamide absorption from the rectum in rats was studied using the recirculating perfusion method with perfusion solutions having different levels in tonicity by changing concentration of sodium chloride and revealed that the absorption was influenced by the apparent transmucosal bidirectional fluid movements.View full abstractDownload PDF (413K)
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