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Volume 27, Issue 8
Displaying 1-42 of 42 articles from this issue
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KEI TSUZURAHARA, YASUTOSHI ONO, KAZUO OGIWARA, TAKASHI MURATA, SHIGEYU ...1979 Volume 27 Issue 8 Pages 1715-1724
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTrimetoquinol (TMQ), like isoproterenol (Iso), inhibited not only the in vitro anaphylactic release of histamine from minced guinea pig lung tissue but also passive cutaneous anaphylaxis (PCA) in rats and guinea pigs and systemic anaphylaxis in guinea pigs. In these inhibitory effects, TMQ was more potent than Iso and other β-adrenergic stimulants (orciprenaline, salbutamol and terbutaline) in vivo, and 1000 times more active than disodium cromoglycate in vitro. In rat PCA, orally administered TMQ was fully effective as early as 5 min after administration and showed a longer duration of action than Iso. Furthermore, TMQ did not greatly affect the vascular permeability, unlike Iso, which markedly inhibited histamine-induced dye leakage on the rat skin, suggesting that the inhibition of PCA by Iso may be partly ascribed to this action on the capillary vessels, and therefore that the anti-anaphylactic activity of TMQ should be that much greater than that of Iso. When rat mast cells were incubated with TMQ, the cellular level of adenosine-3', 5'-cyclic monophosphate (cAMP) was elevated. The inhibition of in vitro histamine release by TMQ and the elevation of cAMP in the mast cells by TMQ and Iso were both antagonized by propranolol, but not by practolol. These results indicate that TMQ and Iso inhibit the anaphylactic reactions by β-adrenergic mechanisms, probably of a β2-type.View full abstractDownload PDF (1039K) -
YUTAKA HIGASHI, NOBORU YATA, AKIRA KAMADA1979 Volume 27 Issue 8 Pages 1725-1732
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of concomitant administration of salicylate on the acetylation and urinary excretion of sulfonamides (sulfanilamide, sulfamethoxazole, sulfadiazine, sulfisoxazole and sulfathiazole) after intravenous administration to rats was studied. The degree of acetylation of sulfamethoxazole in rat urine was found to be significantly decreased by salicylate treatment, but that of sulfathiazole was increased. It was previously found that the eliminations of sulfamethoxazole and sulfathiazole from rat blood were markedly reduced by the concomitant administration of salicylate. To reconcile these apparently conflicting effects of salicylate treatment on the fate of the two sulfonamides, urine samples were collected at intervals and the rate constant of urinary excretion and that of acetylation were calculated employing the elimination rate constant from rat blood. The decrease in the elimination of sulfamethoxazole on salicylate treatment was explained on the basis of a decrease in the acetylation rate constant. However, for sulfathiazole, the decrease in the elimination was a result of a decrease in the excretion rate constant due to the inhibitory effect of salicylate treatment on the excretion of unchanged sulfathiazole.View full abstractDownload PDF (866K) -
HIDEHARU YOKOI, SABURO ENOMOTO1979 Volume 27 Issue 8 Pages 1733-1739
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree varieties of sodium aluminosilicate gels with known distributions of molecular forms of silicic acid were orally administered to rats. One preparation was composed chiefly of low molecular weight silicic acids, another preparation of soluble polysilicic acids, and the third preparation of insoluble polysilicic acids. Urinary silicic acid excretion was regarded as corresponding to silicic acid absorption, after oral administration of these silicate preparations, and the relation between silicic acid absorption and degree of polymerization was studied. Among various silicic acids formed upon acid hydrolysis of silicates in the stomach, orthosilicic acid in particular was absorbed, while polysilicic acids, regardless of solubility, were hardly absorbable. It seems likely that silicic acids are absorbed from the digestive tract through the lipoid membrane pore route, the mechanism being common in the permeation of hydrophilic molecules. The possible mechanism of formation of calculi composed of silicic acid is discussed.View full abstractDownload PDF (777K) -
TOSHIAKI NISHIHATA, NOBORU YATA, AKIRA KAMADA1979 Volume 27 Issue 8 Pages 1740-1746
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of acetoacetic acid (AA) or β-hydroxybutyric acid (HBA), each of which is a component of acetone bodies, on the pharmacokinetic behavior of chlorpropamide (CPA) was studied in order to elucidate the reason for the abnormal behavior of CPA under diabetic conditions. The serum level of CPA in the elimination phase showed a rapid and profound fall immediately after intravenous administration of AA. A change of distribution of CPA in the blood was observed in a normal rabbit. However, under diabetic conditions, with high blood levels of acetone bodies, the effect of AA was temporary. A marked decrease of proximal tubular secretion of CPA was observed under normal conditions after the administration of AA. HBA showed effects similar to those of AA. A marked increase of CPA in red blood cells was observed in the presence of AA or HBA in normal rabbits. These results coincide with those obtained under diabetic conditions. It was concluded that the retardation of urinary excretion and the increase in the distribution of CPA into red blood cells in alloxan diabetic rabbits is mainly due to the presence of acetone bodies in the blood.View full abstractDownload PDF (705K) -
KOJI YAMAKAWA, TSUYOSHI SATOH1979 Volume 27 Issue 8 Pages 1747-1752
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA stereoselective synthesis of (±)-furanofukinol (1a) and (±)-petasalbin (2) starting from the diene adduct (6) is described. Reduction of the diketone (8) with NaBH4 gave the 3β-ol (9) as a main product. Attempted synthesis of 1a from 9, by reduction of 9 with LiAlH4 followed by catalytic reduction, was unsuccessful due to decomposition of 11. Reduction of the diketone (12) gave the 3β-ol (13). The conformations of 13 and its acetate (14) were shown to be non-steroidal (13b and 14b, Fig. 1) by nuclear magnetic resonance (NMR) and nuclear Overhauser effect (NOE) studies. Reduction of 13 with LiAlH4 gave a mixture of 1a and the 6α-ol (15), whereas reduction of 13 with Na metal dissolved in refluxing EtOH gave 1a stereoselectively. On the basis of NMR and infrared (IR) spectral comparisons, 1a and its diacetate (1g) were identical with the natural compounds (1a and 1g, respectively). Reduction of (±)-ligularone (4) under thermodynamic conditions gave 2 stereoselectively. IR and NMR spectral comparisons showed (±)-2 to be identical with petasalbin.View full abstractDownload PDF (650K) -
KAZUO T. SUZUKI, SHINJI TAKENAKA1979 Volume 27 Issue 8 Pages 1753-1758
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRat kidney metallothionein, which contains copper as a major metal, was injected into young female rats to investigate whether the injected kidney metallothionein is degraded and re-synthesis of metallothionein occurs in the kidneys, as in the case of injected liver metallothionein. The changes in the gel filtration profiles of the kidney supernatant fractions with time could be explained by the degradation and re-synthesis of metallothionein in the kidneys. The cadmium and copper liberated from the degraded metallothionein induced the biosynthesis of metallothionein and copper-binding protein (possibly copper-thionein). The re-synthesized metallothionein was rich only in cadmium and zinc, and the half-lives of the two metals were long. On the other hand, the half-life of the copper-binding protein was short. The peak positions of the metallothionein and the copper-binding protein were different on a Sephadex G-75 column. The renal tubularlining cells were severly damaged by the injection of metallothionein. The necrosis and recovery of the kidneys were confirmed by microscopic examinations and by analysis of urinary glucose.View full abstractDownload PDF (727K) -
KENJI MIURA, HIROSHI NAKAMURA, HIROSHI TANAKA, ZENZO TAMURA1979 Volume 27 Issue 8 Pages 1759-1763
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA method is proposed for the simultaneous determination of multiple enzyme activities in a specimen by high performance liquid chromatography. To examine the applicability of the method, the hydrolytic activities of arylsulfatase, β-glucosidase and β-glucuronidase, all having broad optimal pH ranges around 5 were assayed by quantitative determination of 8-hydroxyquinoline (oxine, Ox), 5, 7-dichloro-8-hydroxyquinoline (Di-Cl) and 5-chloro-7-iodo-8-hydroxyquinoline (chinoform, CF), the products released enzymatically from Ox-β-D-glucoside, Di-Cl-sulfate and CF-β-D-glucuronide. The method was applied to rat organs and Bifidobacterium infantis No. 9.View full abstractDownload PDF (589K) -
SHINICHI NAGAI, NORIICHI ODA, ISOO ITO, YOSHIHISA KUDO1979 Volume 27 Issue 8 Pages 1764-1770
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of (1R, 4S)-2-oxobornaneglyoxylic acid (1) with substituted hydrazines gave (4S, 7R)-1-substituted-4, 7-methano-1H-indazole-3-carboxylic acids (2). (4S, 7R)-1-Phenyl-4, 7-methanoindazole-3-ol (8) was synthesized by two independent synthetic routes. (4S, 7R)-N-Substituted-4, 7-methanoindazole-3-carboxamides (4a, b) were tested on an isolated nerve-muscle preparation of bullfrog. Compound 4b caused marked contracture of the muscle.View full abstractDownload PDF (844K) -
SHINICHI NAGAI, NORIICHI ODA, ISOO ITO, YOSHIHISA KUDO1979 Volume 27 Issue 8 Pages 1771-1779
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(4S, 7R)-1 and 2-substituted-4, 7-methanoindazoles were synthesized. The nucleophilic reaction of substituted hydrazines with (1R, 4S)-3-hydroxymethylenebornane-2-one (1) gave corresponding (4S, 7R)-1-substituted-4, 7-methano-1H-indazoles (3). Attempts to synthesize 2-substituted-4, 7-methanoindazoles starting from (1R, 4S)-3-acetoxymethylenebornane-2-one (5a) were unsuccessful. Quarternization of (4S, 7R)-4, 7-methanoindazole (3a) afforded (4S, 7R)-4, 7-methano-1H-indazolium compounds (8, 9 and 10a, b). (4S, 7R)-2-Substituted-4, 7-methanoindazoles (11 and 12) were successfully obtained by the reaction of 3a with acetic anhydride and hydroxylamine-O-sulfonic acid. The structure assignments of the 1 and 2-substituted compounds were made on the basis of their NMR spectra. Pharmacological profiles of newly synthesized compounds were studied in vivo and in vitro. The behavioral symptoms of mice treated with compounds 10a and 10b were serious abnormal gait and catalepsy. The in vitro studies on isolated ileum preparation and isolated heart preparation suggested that compound 10b has effective anticholinergic and antihistaminergic actions.View full abstractDownload PDF (956K) -
HITOSHI TAKAI, AKIRA ODANI, YOSHIO SASAKI1979 Volume 27 Issue 8 Pages 1780-1791
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe 13C chemical shifts of 2-substituted naphthalenes and their 6-methoxy derivatives are considered in terms of empirical parameters, charge densities, and screening tensors. The 13C screening tensors were calculated theoretically using LCGI-MO theory, by the MINDO/2 method. The results were consistent with the experimental data. The 2p electron charge density, the predominant factor governing the calculated 13C chemical shift, also corresponded well with the experimental data.View full abstractDownload PDF (990K) -
TAKUSHI KURIHARA, HIROAKI SHIN, YASUHIKO SAKAMOTO1979 Volume 27 Issue 8 Pages 1792-1796
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new synthetic method using ethyl 3-ethoxymethylene-2, 4-dioxovalerate and phenylhydroxylamine gave 2-acetyl-3-hydroxy-5-phenylmaleimide in moderate yield. The pathway of this reaction is discussed.View full abstractDownload PDF (570K) -
MIYOKO SUZUKI, YOSHIO SASAKI, MAKIKO SUGIURA1979 Volume 27 Issue 8 Pages 1797-1805
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSInclusion compounds of azo dyes which have a naphthalene nucleus were examined by 13C nuclear magnetic resonance (NMR). The azo dyes used form 1 : 1 complexes with cyclodextrin. The guest molecule is uniformly affected by the cavity, as if it were dissolved in a hydrophobic solvent. C-SO3-at the end of the molecule shows the largest shift and can be used as an index of inclusion. Almost all carbons of the guest molecule show low field shifts on inclusion, which are consistent with the 1H NMR behavior. Thus, the shift mechanism may be due not to a simple steric polarization effect, but to hydrophobic interaction with the host molecule. The host molecule is deformed at the glycosidic linkage rather than at the small diameter side of the cavity by the bulky naphthalene nucleus.View full abstractDownload PDF (829K) -
Dibenzotetracyclic Derivatives. II. Synthesis of 9-Aminoalkyl-9, 10-dihydro-9, 10-methanoanthracenesMAKOTO SUNAGAWA, HIROMI SATO, JUNKI KATSUBE, HISAO YAMAMOTO1979 Volume 27 Issue 8 Pages 1806-1812
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA synthesis of 9-aminoalkyl-9, 10-dihydro-9, 10-methanoanthracenes (2) is reported. A key intermediate, 9-formyl-9, 10-dihydro-9, 10-methanoanthracene (4), was synthesized from 9-amino-12-hydroxy-9, 10-dihydro-9, 10-ethanoanthracene (3b) by nitrous acid deamination. The amino-alcohol (3b) was synthesized in 5 steps starting from anthracene-9-carbaldehyde.View full abstractDownload PDF (794K) -
CHIKARA KANEKO, TOSHIHIKO NAITO, MARIMI HASHIBA, HARUE FUJII, MASANORI ...1979 Volume 27 Issue 8 Pages 1813-1819
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo alkaloids, 1-methyl-4-(3-methylbut-2-enyloxy)-2-quinolone (revenine : IIc) and 4-methoxy-1-methyl-2-quinolone (IIa), were synthesized by means of a photochemical rearrangement reaction of the corresponding 4-alkoxy-2-methylquinoline 1-oxide (Ic and Ia), which were conveniently prepared from 4-chloro-2-methylquinoline 1-oxide (XVII), which in turn is readily obtainable from 2-methylquinoline 1-oxide via the 4-nitrated compound (XVIII). The mechanism of the photo-rearrangement reaction of 4-alkoxy-2-methylquinoline 1-oxides (Ia-d) in methanol is discussed.View full abstractDownload PDF (840K) -
SHOICHIRO TAGAMI1979 Volume 27 Issue 8 Pages 1820-1823
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMeprobamate decomposes into NH3, Na2CO3, and a diol compound on heating in 1N NaOH, and CO2 evolved at pH 4.8 can be determined by the use of a CO2 selective electrode without separation from the decomposition solution. A linear calibration curve was obtained within the concentration range of 1×10-4-2.5×10-2M meprobamate. Carbon dioxide in water does significantly influence the potential response, so that this method requires the use of distilled water pre-treated by boiling.View full abstractDownload PDF (498K) -
MASAYUKI TANNO, SHOZO KAMIYA1979 Volume 27 Issue 8 Pages 1824-1829
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-(3-Cyano-1-triazeno) pyridines (III, IX) were synthesized by treating azides (I, VII) with potassium cyanide, followed by acidification with hydrochloric acid. Cyanotriazene potassium salts (II, VIII) gave 4-[3-(N2-hydroxyamidino)-1-triazeno]-pyridines (IVa, Xa) and 4-(3-thiocarbamoyl-1-triazeno) pyridines (IVb, Xb) on reaction with hydroxylamine hydrochloride and with hydrogen sulfide in the presence of ammonia, respectively. The reactions of II and VIII with dialkyl sulfates gave 4-(3-cyano-1-triazene)-1, 4-dihydropyridines (Va, Vb, XIIa, XIIb), which were also derived from the quaternary azides (VIa, VIb, XIIIa, XIIIb). An azourethan (XI) was obtained by treating VIII with ethanol containing a small amount of hydrochloric acid. The arylazo derivatives (XVa, XVb, XVc) were synthesized by treating VIII with a mixture of 2-naphthol or diphenylamine and ethanol containing hydrochloric acid. The reaction of Va and XIIa with hydroxylamine hydrochloride gave 4-[3-(N2-hydroxyamidino)-1-triazeno]-1, 4-dihydropyridine hydrochlorides (XVI, XVII).View full abstractDownload PDF (710K) -
MORIO IKEHARA, YOKO TAKATSUKA, SEIICHI UESUGI1979 Volume 27 Issue 8 Pages 1830-1835
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA dinucleoside monophosphate, 2'-azido-2'-deoxyadenylyl-(3'-5')-2'-azido-2'-deoxyadenosine (II) was synthesized by condensation of the 5'-monomethoxytrityl (IV) and N6, 3'-O-dibenzoyl-5'-phosphoryl derivatives (III) of 2'-azido-2'-deoxyadenosine using DCC as a condensing reagent. The ultraviolet absorption properties of compound II were similar to those of ApA. The circular dichroism (CD) spectrum of II was also similar to that of ApA in pattern, but the magnitudes of the CD bands were about a half of those of ApA. 1H nuclear magnetic resonance signals appeared in the expected position for a dimer, and the dimerization shifts were similar to those of ApA. However, the 3'-linked residue of compound II showed a J1'-2' value significantly higher than that of ApA. These results suggest that compound II takes an anti-anti, right-handed stacked conformation similar to that of ApA, but with decreased stability or with a significantly different stacking geometry.View full abstractDownload PDF (650K) -
HIROKO KIMATA, CHIZUKO HIYAMA, SHOJI YAHARA, OSAMU TANAKA, OSAMU ISHIK ...1979 Volume 27 Issue 8 Pages 1836-1841
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe optimal conditions for conversion of saikosaponins-a (1) and -d (3), the pharmacologically active major saponins of roots of Bupleurum falcatum, into diene-saponins (saikosaponins-b1 (4) and -b2 (6)) was investigated. By means of high performance liquid chromatography (HPLC) on an octadecylsilylated silica gel column, complete separation and highly sensitive quantitative analysis of these diene-saponins, which exhibit characteristic ultraviolet maxima, were possible, offering a rapid and selective procedure for the determination of 1 and 3 in commercial samples of Bupleuri radix. Some of the crude drugs on the Japanese market were evaluated by this procedure and it was found that the HPLC pattern of "Chiku-Saiko" imported from Korea was different from those of other crude drugs and cultivated B. falcatum, but similar to that of roots of B. longeradiatum, supporting the morphological comparison of Konoshima et al.View full abstractDownload PDF (665K) -
KATSUMI TABEI, ETSUKO KAWASHIMA, TETSUZO KATO1979 Volume 27 Issue 8 Pages 1842-1846
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of γ-bromoacetoacetyl bromide (1) with N-arylhydroxylamines (2) afforded N-(γ-bromoacetoacetyl)-N-arylhydroxylamines (3), which were treated with sodium methoxide to give 2-aryltetrahydro-2H-1, 2-oxazine-3, 5-dione (4). Treatment of 3 with hydroxylamine directly afforded the 5-oxime derivatives of 4 (7), which could be transformed to 4 by mild hydrolysis with dilute mineral acid.View full abstractDownload PDF (666K) -
TOZO FUJII, HIROSHI KOGEN, SHIGEYUKI YOSHIFUJI, KIYOMI IGA1979 Volume 27 Issue 8 Pages 1847-1856
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn the basis of chemical and spectroscopic evidence, the structure 5 has been assigned to an unsaturated lactam acid of mp 126-127° (slight effervescence) which was temporarily expressed by the structure 6 previously. The chemical evidence obtained here includes the results of the following reactions : esterifications of the lactam acid 5 to the ethyl ester 8 and to the methyl ester 9 ; alkaline hydrolyses of the two esters 8 and 9 to the starting acid 5 at room temperature ; conversion of 9 into the lactam amide 12 ; LiAlH4 reduction of 9 to the lactam alcohol 10 ; chromic acid oxidation of 10 to the starting acid 5 ; alkaline hydrolyses of the esters 8 and 9 to a mixture of 5 and the isomeric lactam acid 7 at a higher temperature ; base-catalyzed isomerization of 5 to 7 or vice versa, reaching equilibrium ; thermal decarboxylation of 5 to a mixture of 13 and 14 ; base-catalyzed isomerization of 13 to 14. The assigned structures of the lactam derivatives thus obtained were also supported by their ultraviolet, infrared, proton magnetic resonance, and C-13 nuclear magnetic resonance spectra.View full abstractDownload PDF (1085K) -
SHIGERU AONUMA, YASUHIRO KOHAMA, KUNIHISA AKAI, TOMINORI MORITA, SHIGE ...1979 Volume 27 Issue 8 Pages 1857-1863
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of oxytocin on the beating properties of rat myocardial cells in cultures supplemented with serum, and on the spreading functions in serum-free culture were investigated. Oxytocin significantly increased the beating rates of single cells and cell clusters, and made quiescent single cells beat in a 2-day culture with Eagle's minimum essential medium supplemented with 10% bovine serum. The spontaneous activity of myocardial cells increased by oxytocin was not inhibited by the addition of propranolol, contrary to the case with epinephrine. Oxytocin improved the arrhythmia of myocardial cells which showed partial or continuous cellular fibrillation and mild irregular beating induced by lowering the potassium concentration of culture media. As for the spreading functions, oxytocin increased myosin ATPase activity and protein synthesis, increasing the spreading phenomenon, but did not affect the amounts of ATP and phosphocreatine, or the nucleic acid synthesis of myocardial cells cultured with the sample in serum-free medium for 2 days.View full abstractDownload PDF (766K) -
SHIGEO IKEGAWA, YOSHIHIRO HINO, MASAYUKI SUNAGAWA, TOSHIO NAMBARA1979 Volume 27 Issue 8 Pages 1864-1870
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to clarify the stereochemistry of hydrogen loss from the C-2 position during microbial transformation of 5β-pregnane-3, 11, 20-trione into the Δ1-unsaturated compound, the stereospecific synthesis of epimeric C-2 deuterated substrates has been carried out. A key intermediate, 5β-pregn-2-ene-11α, 20β-diol diacetate, was obtained from the readily available 11α-hydroxyprogesterone through two synthetic routes. The trans-diaxial opening of the 2β, 3β-epoxide with lithium aluminum deuteride provided the 2α-d1-3β-ol. Deuterioboration of the Δ2-olefin and subsequent oxidation of the organoborane afforded the 2α-d1-3β-ol. On oxidation with chromium trioxide-pyridine complex, the epimeric 2-d1-5β-pregnane-3β, 11α, 20β-triols were converted to the desired 2-d1-5β-pregnane-3, 11, 20-triones.View full abstractDownload PDF (902K) -
HIROSHI SAKAGUCHI, HIROSHI ANZAI, KIMIO FURUHATA, HARUO OGURA, YOICHI ...1979 Volume 27 Issue 8 Pages 1871-1880
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe crystal structure of the copper (II) complex of 2-hydrazino-4-hydroxy-6-methylpyrimidine (LH) has been determined from three-dimensional X-ray diffractometer data by heavy atom Fourier methods. Crystals of [Cu (LH)2 (H2O)] Cl2·2H2O are triclinic with unit cell dimensions a=10.020 (2), b=14.384 (2), c=7.205 (1) Å, α=104.63 (2)°, β=111.04 (1)°, γ=84.93 (2)°, space group P 1, and Z=2. Block-diagonal least-squares refinement using 3126 independent reflections yielded an R value of 0.062. There are two mirror-image complex molecules in a unit cell. Each copper (II) complex has five coordinated bonds and assumes a distorted square pyramid structure. The two ligand molecules, (LH)2 are trans coordinated to the copper (II) ion through nitrogen atoms N3 of the pyrimidine rings and also through the amino nitrogen atoms of the hydrazino groups. In each copper (II) complex, the one apical coordination site is occupied by the water oxygen atom. The hydroxyl group at C4 of the pyrimidine ring takes the keto form, since the hydrogen atom of the hydroxyl group transfers to N1 of the ring. The chloride ions are not directly hydrogen bonded to the N1 atoms of the pyrimidine bases, but are bound to the apical water oxygen atoms. The pyrimidine rings in the crystals are not stacked in parallel but are inclined at an angle of 18.9 or 18.8°.View full abstractDownload PDF (904K) -
KAZUTAKE SHIMADA, TOSHIO NAMBARA1979 Volume 27 Issue 8 Pages 1881-1886
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe occurrence of new cardiotonic steroid conjugates in the skin of a tropical toad, Bufo marinus (L.) SCHNEIDER, is reported. These substances were separated by chromatography on Amberlite XAD-4 resin and silica gel, high-performance liquid chromatography, and gel chromatography on Sephadex LH-20. The sulfated bufogenins, marinobufagin 3-sulfate and resibufogenin 3-sulfate, were characterized by degradative and synthetic means. In addition, the structures of two new bufotoxins were elucidated as marinobufagin 3-pimeloylarginine ester and telocinobufagin 3-suberoylarginine ester.View full abstractDownload PDF (760K) -
MASAYUKI NAKAGAKI, MASATOSHI INOUE, SUZUKO MITOGUCHI, TOSHIMASA ISHIDA1979 Volume 27 Issue 8 Pages 1887-1892
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs a part of our studies on the conformational analysis of calcium glycerophosphate, empirical potential energy calculations were carried out to investigate the conformational features of α- and β-glycerophosphates. The energy terms included in the total energy expression consist of nonbonded, electrostatic and torsional energies. In this calculation, the values of torsion angles are parameterized and optimized by means of the Powell algorithm. We obtained four stable conformations for α-glycerophosphate and three for β-glycerophosphate. The conformational features of glycerophosphates could be summarized as follows ; the conformation of α-d-glycerophosphate is characterized by the glycerol backbone chain (Ψ2, Ψ3) corresponding to trans-gauche (+), and that of β-glycerophosphate is characterized by the linkage of glycerol and phosphate groups (Ф5) corresponding to gauche (-).View full abstractDownload PDF (608K) -
SHOJI TAKEMURA, YASUYOSHI MIKI, FUSAO KOMADA, KEIKO TAKAHASHI, ARITOMO ...1979 Volume 27 Issue 8 Pages 1893-1900
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA common conformation was assumed to be involved in the potent muscarinic activities of L (+)-muscarine, acetylcholine, and (+)-trans-2S-acetoxycyclopropyl-1S-trimethyl-ammonium. The conformation of other muscarinic agents was also considered from this point of view ; three types of quaternary salts having semi-rigid piperidine ring structures which satisfy the hypothetical requirements were synthesized, and their muscarinic activities were examined. These synthetic compounds showed selective muscarinic activity.View full abstractDownload PDF (841K) -
KUNIYOSHI TANAKA, KEIZO MATSUO, YOSHIHIKO NAKAIZUMI, YASUNORI MORIOKA, ...1979 Volume 27 Issue 8 Pages 1901-1906
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3-Acyltetronic acids and their copper complexes, which possess a tricarbonylmethane structure, were prepared and tested for antimicrobial activity. 3-(1-Iminoalkyl) tetronic acids and their copper complexes were prepared and tested for inhibitory activity towards chlorophyll development of plants. It was found that the 3-decanoyl group was essential for the appearance of the former activity and the 3-(1-iminoethyl) group for that of the latter.View full abstractDownload PDF (703K) -
YUICHIRO YABE, CHIEKO MIURA, HIROYOSHI HORIKOSHI, HIROKO MIYAGAWA, YOS ...1979 Volume 27 Issue 8 Pages 1907-1911
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeven analogs of luteinizing hormone-releasing hormone (LH-RH), in which the Trp residue at position 3 was replaced by various methyltryptophans and 1-ethyltryptophan, were synthesized and their LH-releasing activities were evaluated. All of these analogs showed reduced hormonal activity compared with synthetic LH-RH.View full abstractDownload PDF (685K) -
KEISUKE KAWASHIMA, HIROSHI ITOH, MUNEJI MIYOSHI, ICHIRO CHIBATA1979 Volume 27 Issue 8 Pages 1912-1916
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe antioxidant activities of branched-chain amino acid derivatives, such as dipeptides and amino alcohols, were evaluated by means of the active oxygen method. Dipeptides containing a branched-chain amino acid showed higher antioxidant activities than did those having no branched-chain amino acid. An N-terminal branched-chain amino acid in dipeptides was preferable to a C-terminal one for antioxidant activity. A free N-terminal amino group was also found to be important for the appearance of antioxidant activity.View full abstractDownload PDF (573K) -
YOSHIFUMI MAKI, TAKASHI FURUTA, MIKIO SUZUKI1979 Volume 27 Issue 8 Pages 1917-1918
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotolysis of ethyl α-nitro-β-(3-indolyl) propionate resulted in the formation of ethyl α-hydroxyimino-β-(2-oxindol-3-yl) propionate.View full abstractDownload PDF (346K) -
HIROTERU SAYO1979 Volume 27 Issue 8 Pages 1919-1922
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Diethylaminoantipyrine cation radical (II) was generated by the anodic oxidation of 4-diethylaminoantipyrine (I) in acetonitrile containing 0.1M NaClO4 at a glassy-carbon anode, and the rate of disappearance of II in aqueous acetonitrile solutions was measured by spectrophotometry. In aqueous acetonitrile solutions of pH 7.4 and 10.4, II decayed in a first-order manner, and the first-order rate constant obtained increased with increasing concentration of the buffers and hydroxyl ions and with decreasing concentration of NaClO4 added. On the other hand, in a solution containing 0.1M HClO4, II decayed in a second-order manner. The second-order rate constant obtained was independent of the ionic strength of the solution and decreased with increasing concentration of acetonitrile. A mechanism for the decomposition of II is suggested.View full abstractDownload PDF (514K) -
YASUTAKA NAGAI, AKIRA IRIE, HITOSHI UNO, SHINSAKU MINAMI1979 Volume 27 Issue 8 Pages 1922-1926
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe alkylation of 2-substituted 2, 3, 4, 5-tetrahydro-1H-pyrido [4, 3-b] indoles (1) with sodium amide and alkyl halide in non-polar solvents proceeded most smoothly when the substituent in the 2 position was a benzyl group, and gave 5-alkyl-1, 2, 3, 4-tetrahydropyrimido [1, 6-a] indoles (2) and 5-alkyl-tetrahydropyrido [4, 3-b] indoles (3). The ratio of 2 to 3 depended on the halide employed. The tetrahydropyrimido [1, 6-a] indole derivatives (5) with a 3-(p-fluorobenzoyl) propyl group in the 2 position were also prepared.View full abstractDownload PDF (558K) -
JUNICHI GOTO, KAZUHIKO SUZAKI, TOSHIO NAMBARA1979 Volume 27 Issue 8 Pages 1926-1931
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe glucuronides, sulfates, glucosides and N-acetylglucosaminides of cholesterol and epimeric 5α-cholestan-3-ols have been synthesized. The formation of a β-glucoside linkage was readily achieved by means of the Koenigs-Knorr reaction with the corresponding α-acetohalosugar, employing cadmium carbonate as a catalyst. The preparation of 6, 7α, 7β-d3-cholesterol glucuronide is also described.View full abstractDownload PDF (791K) -
HARUNORI YASUO, MAMORU SUZUKI, NAOTO YONEDA1979 Volume 27 Issue 8 Pages 1931-1934
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSVarious α-substituted α-imino acids (6) were synthesized in good yields by the reaction of methyl α-substituted α-isocyanoacetates with alkylene bromides in the presence of sodium hydride, followed by cyclization and hydrolysis.View full abstractDownload PDF (541K) -
ISAO KITAGAWA, YOSHIHIRO HAMAMOTO, MOTOMASA KOBAYASHI1979 Volume 27 Issue 8 Pages 1934-1937
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn the basis of chemical and physicochemical evidence, a sulfonoglycolipid isolated from the shell of the sea urchin Anthocidaris crassispina A. AGASSIZ has been shown to be a 96 : 4 mixture of 1'-O-palmitoyl-3'-O-(6-sulfo-α-D-quinovopyranosyl) glycerol and its myristoyl counterpart.View full abstractDownload PDF (518K) -
ATSUKO NODA, KENJI MATSUYAMA, SHUHWAI YEN, NOZOMU OTSUJI, SADAO IGUCHI ...1979 Volume 27 Issue 8 Pages 1938-1941
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe liberation of hydrazine from hydralazine was demonstrated in rabbit urine, in rat plasma and in a rat enzyme system. The identification of hydrazine in rabbit urine was performed by comparison of the gas chromatogram and mass spectrum of its benzalazine derivative with those of an authentic sample. Small amounts of hydrazine extracted from rat plasma and the rat enzyme system were detected by mass fragmentography using 15N-hydrazine.View full abstractDownload PDF (456K) -
YUKO HIRAI, TADASHI YASUHARA, HISANOBU YOSHIDA, TERUMI NAKAJIMA, MASAH ...1979 Volume 27 Issue 8 Pages 1942-1944
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe new mast cell degranulating peptide "mastoparan" was isolated from the venom of Vespula lewisii (Vespid wasp) and the peptide was synthesized chemically. Mastoparan is tetradecapeptide amide constituted of the restricted amino acid and the repeated sequence.View full abstractDownload PDF (410K) -
YUKO HIRAI, MANABU KUWADA, TADASHI YASUHARA, HISANOBU YOSHIDA, TERUMI ...1979 Volume 27 Issue 8 Pages 1945-1946
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe haemolytic factor in the venom of Japanese hornet (Vespa xanthoptera) was identified as the new peptide consisting of the following sequence ; Ile-Asn-Trp-Lys-Gly-Ile-Ala-Ala-Met-Ala-Lys-Lys-Leu-Leu-NH2 The structure is closely related to mastoparan, and the peptide revealed mast cell degranulating activity and released also serotonin from platelets. The peptide was named "Mastoparan-X."View full abstractDownload PDF (361K) -
MIYOJI HANAOKA, KAZUYOSHI NAGAMI, TAKESHI IMANISHI1979 Volume 27 Issue 8 Pages 1947-1948
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(±)-α- and (±)-β-Hydrastine (3 and 4) were synthesized from (±)-ophiocarpine (1) and (±)-13-epiophiocarpine (2), respectively, with complete retention of configuration through a regioselective C8-N bond cleavage.View full abstractDownload PDF (336K) -
SACHIKO YAMADA, KEIKO NAKAYAMA, HIROAKI TAKAYAMA, AKIKO ITAI, YOICHI I ...1979 Volume 27 Issue 8 Pages 1949-1950
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe precise structures of the biologically potent endoperoxides derived from vitamin D2, vitamin D3, and their benzoates by dye sensitized photo-oxidation were established by X-ray analysis as well as by analysis of their circular dichroism spectra.View full abstractDownload PDF (346K) -
MASARU KOBAYASHI, ATSUSHI TOMIOKA, TAKAAKI HAYASHI, HIROSHI MITSUHASHI1979 Volume 27 Issue 8 Pages 1951-1953
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new marine C28 sterol was isolated from the soft coral, Sarcophyton glaucum, and its structure was proposed as (22E)-23-methylcholesta-5, 22-dien-3β-ol on spectral evidences, especially by the comparison of its 13C-NMR chemical shifts with those of 23, 24-dimethylcholesta-5, 22-dien-3β-ol, which is present in the same soft coral.View full abstractDownload PDF (418K) -
TERUKO HASHIMOTO, TOMOE NEGISHI, TETSUTO NAMBA, SHOHEI HAYAKAWA, HIKOY ...1979 Volume 27 Issue 8 Pages 1954-1956
Published: August 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSQuinoline derivatives and analogs were surveyed for their mutagenicity using the Salmonella/microsome assay. 4-Methylquinoline, 4-methylquinoline 1-oxide, quinoxaline 1-oxide, quinoxaline 1, 4-dioxide, 2, 3-dimethylquinoxaline 1, 4-dioxide, benzo [f] quinoline, 1-methylbenzo [f] quinoline, and 4-methylbenzo [h] quinoline were mutagenic on S. typhimurium TA 100 in the presence of the rat liver 9000×g supernatant ("S-9 mix"). Quinoxaline 1-oxide, quinoxaline 1, 4-dioxide, and 2, 3-dimethylquinoxaline 1, 4-dioxide were also mutagenic on TA 100 in the absence of S-9 mix. 2-Methylquinoxaline was mutagenic on strain TA 98 in the presence of S-9 mix. Among these mutagenic compounds, quinoxaline 1, 4-dioxide was the strongest mutagen. The following compounds showed no significant mutagenicity on TA 98 and TA 100 both in the presence and absence of S-9 mix : 2-methylquinoline, 2, 4-dimethylquinoline, quinoline-2-carboxamide, 4-methylquinoline-2-carboxamide, N-methylquinoline-2-carboxamide, N, 4-dimethylquinoline-2-carboxamide, 2-(2-pyrazinyl) quinoline, 2-(5-pyrimidinyl) quinoline, benzo [h] quinoline, 1, 10-phenanthroline, quinoline 1-oxide, 2-methylquinoline 1-oxide, 2, 4-dimethylquinoline 1-oxide, isoquinoline, 3-methylisoquinoline, isoquinoline-1-carboxamide, 4-chloroquinazoline, quinoxaline, 2, 3-dimethylquinoxaline, 3-methylquinoxaline-2-carboxamide, 2, 3-bis (2-pyridyl)-quinoxaline and acridine.View full abstractDownload PDF (463K)
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