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Volume 27, Issue 5
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TSUTOMU KAMEYAMA, MAKOTO UKAI1979 Volume 27 Issue 5 Pages 1063-1068
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThis investigation was carried out in an attempt to ascertain whether all narcotic analgesics produce the Straub tail reaction (STR), and whether the morphine-induced STR could be depressed by centrally acting muscle relaxants. Morphine, oxycodone and levorphanol elicited the STR dose-dependently but codeine, pethidine and pentazocine gave only slight STR. The peak time of the STR was 30 min after the administration of morphine. Intracerebral injection of morphine evoked the STR, but not markedly. Naloxone and pentazocine depressed the morphine-induced STR considerably. Chlordiazepoxide, diazepam, oxazepam, carisoprodol, chlormezanone, chlorzoxazone, meprobamate, orphenadrine, chlorpromazine, perphenazine and haloperidol also reduced the morphine-induced STR markedly. The morphine-induced STR was inhibited noticeably by intracerebral or systemic injection of baclofen and difenamizole. The intracerebral dose of baclofen required for this inhibition was as low as approximately one-thousandth of that by systemic administration. These findings suggest that the morphine-induced STR is positively depressed by centrally acting muscle relaxants.View full abstractDownload PDF (691K) -
MASATOSHI HARADA, YUKIHIRO OZAKI, HIROSHI OHNO1979 Volume 27 Issue 5 Pages 1069-1074
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of six indole alkaloids on parasympathetic ganglionic transmission were studied in a preparation of the guinea pig urinary bladder in situ. The effect of hirsutine on spontaneous movement of the organ was also examined. Among these alkaloids, gardneramine and hirsutine most potently inhibited the contraction of the urinary bladder induced by electrical stimulation of the pelvic nerves. Their potency was about one-half of that of hexamethonium. The effect of gardneramine was of short duration. Both alkaloids depressed the contraction induced by intraarterial dimethylphenylpiperazinium, with no antagonizing action to the acetylcholine-induced contraction. Hirsutine showed a local anesthetic action in the isolated frog sciatic nerve preparation, while other alkaloids had only a weak effect. Hirsutine, isorhynchophylline, and gardnerine elevated the tone of the spontaneous movement of the organ and augmented its amplitude. The stimulating action of hirsutine was not affected by pretreatment with tetrodotoxin, atropine, diphenhydramine, or hexamethonium.View full abstractDownload PDF (696K) -
JUN WATANABE, HIROSHI OKABE, KENJI MIZOJIRI, YOSHITSUGU NAKAJIMA, KOIC ...1979 Volume 27 Issue 5 Pages 1075-1084
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe drug was well absorbed from the intestinal tract, and the bulk of it was excreted in the urine and feces. Biliary excretion was significant, and the existence of enterohepatic circulation was considered likely. After intravenous injection, elimination of radioactivity from the blood and various tissues, except for fat, was rapid for 2 hr, then became slower. Elimination of unchanged drug from the blood was very fast. Repeated oral doses did not changed the excretion and distribution features as compared to a single oral dose. Significant accumulation of radioactivity was not caused by repeated doses of 14C-labeled perisoxal. Three oxidized metabolites, p-hydroxyperisoxal, m-hydroxyperisoxal and 4-hydroxyperisoxal, were identified. Excretion of hydroxyperisoxals in the urine (free and conjugates) was greater than that of perisoxal itself.View full abstractDownload PDF (952K) -
KEIICHI ONO, JUNKI KATSUBE1979 Volume 27 Issue 5 Pages 1085-1093
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNine diastereoisomers containing a hydroxy or carbonyl group on the cycloheptane ring of bencyclane were synthesized. Configurational analysis of γ-hydroxybencyclane was attempted in order to determine the configuration of the major bencyclane metabolite.View full abstractDownload PDF (875K) -
MASAKAZU SAKAGUCHI, YOSHIHISA MIYATA, HARUO OGURA, KINJI GONDA, SHOZO ...1979 Volume 27 Issue 5 Pages 1094-1100
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn connection with studies of nucleoside analogs, the interactions of Schiff bases with HgCl2, PdCl2, and other metal halides (MgCl2, CaCl2, BaCl2, SrCl2, ZnCl2, and CdCl2) in dimethyl sulfoxide were examined at room temperature using time-dependent electron spin resonance and nuclear magnetic resonance spectroscopy. Pteridine or theophylline derivatives were obtained from the reaction of Schiff bases with HgCl2 or PdCl2 via radical or ionic intermediates. On the other hand, in the cases of other metal halides, the products could not be isolated. This reaction may be a useful tool for the preparation of nucleoside analogs.View full abstractDownload PDF (626K) -
TETSUYA NAKAMURA, HIDEYUKI SANMA, SUKEHIRO IMABAYASHI, YOSHIO SAWA, KI ...1979 Volume 27 Issue 5 Pages 1101-1105
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe distribution of exogenous ubiquinone-10 in canine plasma was examined using deuterium-labeled ubiquinone-10 in conjunction with a computerized gas chromatographmass spectrometry system. Electron transport enzymes in canine leucocytes were also studied. An increase in the plasma level of exogenous ubiquinone-10 did not affect the level of endogenous ubiquinone-10, and it was reflected in increased activities of the electron transport enzymes (succinate dehydrogenase Co Q reductase, succinate cytochrome c reductase and succinate oxidase) in leucocytes.View full abstractDownload PDF (583K) -
HITOSHI SEKIKAWA, KEIJI ITO, TAKAICHI ARITA, RYOHEI HORI, MASAHIRO NAK ...1979 Volume 27 Issue 5 Pages 1106-1111
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of sodium carboxymethylcellulose (CMC), sodium arginate (SA), methylcellulose (MC) and polyvinylpyrrolidone (PVP) on the intestinal absorption of acetaminophen in situ were investigated in rats. Among the macromolecular additives, only PVP exhibited an inhibitory effect on the absorption of the drug. Studies in vitro (solubility and dialysis experiments) showed that there is an interaction between acetaminophen and PVP. The inhibitory effect of PVP on the intestinal absorption of acetaminophen was suppressed by the addition of urea. Dialysis data showed that urea tends to reduce the binding between acetaminophen and PVP.View full abstractDownload PDF (657K) -
HIDEAKI UMEYAMA, TOMOKO NOMOTO1979 Volume 27 Issue 5 Pages 1112-1119
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA molecular orbital study of molecular interactions between formic acid and ammonia was performed using the ab initio LCAO-SCF-MO method. As primitive functions, the STO-3G basis set, in which valence properties are comparable to those of the STO set, was used. The interaction energies between NH4+ and HCOO-, between NH4+ and HCOOH, between NH3 and HCOO-, and between NH3 and HCOOH were calculated. For the NH4+-HCOO- complex, the structure containing two hydrogen bonds and in which the C2v axis of NH4+ coincides with that of HCOO- was the most stable. For the complex NH4+-HCOOH, the structure in which the NH bond of NH4+ forms a hydrogen bond with the carbonyl oxygen was more stable. For the complex of NH3 and HCOO-, O of HCOO- and the NH bond of NH3 form a linear hydrogen bond as the most stable structure. For the NH3-HCOOH complex, the structure in which the nitrogen lone pair of NH3 forms a linear hydrogen bond with the OH bond of HCOOH was the most stable. Those four structures are discussed in connection with the interaction between lysine and glutamate (or aspartate), and the hydrolysis of esters, taking account of the interaction energies between HCOOH and H2O and between HCOO- and H2O, and the stabilities in vacuum and in nonpolar solvents.View full abstractDownload PDF (754K) -
KAZUMASA HIRAUCHI, TAMEYUKI AMANO1979 Volume 27 Issue 5 Pages 1120-1124
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSubstituent effects on the fluorescence and phosphorescence of 4'-substituted 4-nitrodiphenylamines and 2-(substituted anilino)-5-nitropyridines at 77°K were examined, and satisfactory linear relationships between Hammett's substituent constant σ and the lowest excited singlet energy levels, the lowest excited triplet energy levels, and the triplet decay constants of the compounds were obtained.View full abstractDownload PDF (503K) -
YOKO SAKIYA, YOSHINOBU AKADA, SADAKO KAWANO, YOSHIKO MIYAUCHI1979 Volume 27 Issue 5 Pages 1125-1129
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA method was established by which glycyrrhizin and glycyrrhetinic acid present in plasma can be extracted with methanol and then separated and determined quantitatively within 10 min by means of high-speed liquid chromatography. Using this method, glycyrrhizin and glycyrrhetinic acid added to the plasma were recovered to satisfactory extents. An in situ recirculating perfusion technique showed that G is absorbed in rat small intestine in an apparent first-order process. There was no detectable amount of glycyrrhetinic acid in the blood after bolus injection of glycyrrhizin into the portal vein, althouth glycyrrhetinic acid was present in a detectable amount in the blood after oral administration. Since it is water-soluble and has a high molecular weight, glycyrrhizin is probably absorbed in the small intestine in the form of glycyrrhetinic acid. With the decline of glycyrrhetinic acid in the blood, there was a rise in the blood level of a substance which exhibited the same chromatographic behavior as glycyrrhizin. This substance appears to be a glucuronic acid conjugate formed as a metabolite of glycyrrhetinic acid, although it is not clear whether it is a mono-or diglucuronic acid conjugate or a mixture of the two. Glycyrrhizin injected into the portal vein was eliminated from the blood only slowly.View full abstractDownload PDF (619K) -
HIROSHI TAKAHASHI, NORIYUKI NIMURA, HARUO OGURA1979 Volume 27 Issue 5 Pages 1130-1136
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReactions of various amino compounds with D-glycosyl-and D-gluconylisothiocyanates gave the corresponding thioureides in good yields. Attempts to cause the ring closure of N-glucopyranosyl-N'-phenyl thioureide with methyl cyanoacetate or methyl propiolate under acidic conditions were unsuccessful.View full abstractDownload PDF (663K) -
HIROSHI TAKAHASHI, KAZUYOSHI TAKEDA, NORIYUKI NIMURA, HARUO OGURA1979 Volume 27 Issue 5 Pages 1137-1142
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of glycosyl isothiocyanate (1a) with amino acids such as ethyl L-phenylalaninate hydrochloride, ethyl L-leucinate hydrochloride and ethyl β-alaninate hydrochloride afforded glycosyl thioureides (3a. b, c) in good yields. Reaction of D-gluconyl isothiocyanate (1c) with amino acids (glycine, β-alanine, γ-aminobutyric acid, ε-aminocaproic acid) or p-aminobenzoic acid gave the corresponding D-gluconamides (4a, b, c, d) and/or D-gluconyl thioureides (5a, b, 7, 8). Treatment of 1a, b, c with 6-aminopenicillanic acid (6-APA) or ampicillin in the presence of triethylamine gave triethylammonium 6-(substituted thioureido) penicillanates (9a, b, c) and triethylammonium 6-(D-glycosyl thioureido) benzylpenicillanates (10a, b). The reaction between 1c and phenacyl 6-APA afforded phenacyl 6-(D-gluconyl thioureido) penicillanate (9d).View full abstractDownload PDF (687K) -
HIROSHI TAKAHASHI, NORIYUKI NIMURA, HARUO OGURA1979 Volume 27 Issue 5 Pages 1143-1146
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of glycosyl isothiocyanates (1a, b, c) with anthranilic acid gave corresponding glycosyl thioquinazolines (3a, b, c) in the presence of zinc chloride in excellent yields. The reaction performed in the absence of zinc chloride afforded the intermediate glycosyl thioureides (2a, b) along with the cyclized compounds. However, similar treatment of 1a with 2-amino-3-carboethoxypyridine did not give the corresponding glycosyl pyridopyrimidine (5a), but glycosyl thioureide (4a) was obtained in good yield. Attempted ring closure of 4a under neutral or acidic conditions failed. Similar reactions of 1a, b, and c with 3-aminopyrazole-4-carboxylic acid in the presence of zinc chloride afforded corresponding pyrazolo [4, 3-e] pyrimidine glycosides (6a, b and c) in fair yields.View full abstractDownload PDF (480K) -
HIROSHI TAKAHASHI, NORIYUKI NIMURA, HARUO OGURA1979 Volume 27 Issue 5 Pages 1147-1152
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of glycosyl isothiocyanates (5a-c) with 2-aminopyridine or 2-amino-4-picoline gave N-glycosyl-N'-(pyrid-2-yl) thioureide (6a) or N-glycosyl-N'-(4-methylpyrid-2-yl) thioureide (6b), respectively, in good yields ; cyclized products were not obtained. On the other hand, the reaction of glycosyl isothiocyanates (5a-c) with ethyl 3-aminocrotonate yielded ethyl 3-amino-2-glycosylthiocarbamoylcrotonates (7a-c) and glycosylaminoisothiazoles (8a-c). A similar reaction between 5a-c and 6-amino-1, 3-dimethyluracil afforded glycosylaminoisothiazolo [3, 4-d] pyrimidines (10a-c) in excellent yields.View full abstractDownload PDF (617K) -
HIROSHI TAKAHASHI, NORIYUKI NIMURA, NAKA OBATA, HITOMI SAKAI, HARUO OG ...1979 Volume 27 Issue 5 Pages 1153-1158
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReactions of glycosyl isothiocyanates (1a, b, c) with diamines such as o-phenylenediamine, 2, 3-diaminopyridine or 5, 6-diamino-1, 3-dimethyluracil gave the corresponding glycosyl thioureides in good yields. Glycosyl thioureides were converted into N-glycosylaminobenzimidazoles (5a, b, c), N-glycosyl-3-deazapurine (6a) or N-glycosylaminotheophyllines (7a, b, c) in excellent yields through a cyclodesulfurization reaction.View full abstractDownload PDF (587K) -
YASUTAKA NAGAI, HITOSHI UNO, SUSUMU UMEMOTO1979 Volume 27 Issue 5 Pages 1159-1168
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 1-substituted piperidine and 1, 2, 3, 6-tetrahydropyridine derivatives bearing an aroylethyl group in the 2-position or a p-pluorobenzoyl group in the 4-position were synthesized for pharmacological testing. 1-Ethyl-2-[2-(p-fluorobenzoyl) ethyl] piperidine (6e) exhibited the most potent neuroleptic activity and its pharmacological profile is similar to that of thioridazine (I). Among the butyrophenone derivatives containing their side chain in the piperidine ring, 1-ethyl-3-(p-fluorophenacyl) piperidine (III) showed the most potent activity.View full abstractDownload PDF (920K) -
TOSHIO TSUJIMOTO, TOSHIRO NOMURA, MAKIKO IIFURU, YOSHIO SASAKI1979 Volume 27 Issue 5 Pages 1169-1175
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS^<13>C chemical shifts of 4-substituted pyridazines and 2-substituted pyrazines, together with 1H chemical shifts of the former compounds were measured. Linear correlations of the 13C and 1H chemical shifts of 4-substituted pyridazines with those of monosubstituted benzenes and monosubstituted pyridines and with substituent constants σπ were found. In addition, similar trends were noted for 2-substituted pyrazines. Chemical shifts of pyridazines and pyrazines can be predicted on the basis of these relationships.View full abstractDownload PDF (614K) -
TETSUZO KATO, NOBUYA KATAGIRI, RENZO SATO1979 Volume 27 Issue 5 Pages 1176-1180
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of diketene with diazoacetone (2) in the presence of benzophenone under irradiation afforded trans-1-acetyl-5-oxo-4-oxaspiro [2, 3] hexane (3) in 22% yield. Similarly, the photolysis of diketene and 2-diazoesters such as ethyl 2-diazo-3-oxo-butanoate (4a) and ethyl 2-diazo-3-oxohexanoate (4b), followed by treatment with absolute methanol saturated with dry hydrogen chloride gave diesters ; e.g., methyl 3, 6-dioxo-5-ethoxycarbonylhexanoate (8a) (39%) and methyl 3, 6-dioxo-5-ethoxycarbonylnonylate (8b) (30%), and/or furan derivatives ; e.g., 3-ethoxycarbonyl-5-methoxycarbonylmethyl-2-methylfuran (9a) (35%) and 3-ethoxycarbonyl-5-methoxycarbonylmethyl-2-propylfuran (9b) (33%). A similar reaction of diketene with di-tert-butyl diazomalonate (10) gave rise to dimethyl 2-methoxycarbonyl-4-oxohexane-1, 6-dioate (12) in 58% yield.View full abstractDownload PDF (562K) -
TETSUZO KATO, YUJI SUZUKI, MASAYUKI SATO1979 Volume 27 Issue 5 Pages 1181-1185
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotolysis of acyl azides (1, 10) in diketene was investigated. Irradiation of a mixture of benzoyl azide (1a) and diketene in dichloromethane gave 1-benzoyl-4-hydroxy-3-pyrrolin-2-one (2a) in 17% yield. Similarly, reaction of diketene with p-anisoyl azide (1b), p-toluoyl azide (1c), p-chlorobenzoyl azide (1d) and ethyl azidoformate (10) gave the corresponding pyrrolinones (2b, 2c, 2d, and 11) in 7-22% yields.View full abstractDownload PDF (616K) -
TETSUZO KATO, TAKUO CHIBA, TSUGIO OKADA1979 Volume 27 Issue 5 Pages 1186-1189
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSVilsmeier reactions of ethyl 2-benzimidazoleacetate (4), ethyl 2-benzothiazoleacetate (5), and ethyl 2-benzoxazoleacetate (6) gave ethyl α-(dimethylaminomethylene)-2-benzimidazoleacetate (7), ethyl α-(dimethylaminomethylene)-2-benzothiazoleacetate (8), and ethyl α-(dimethylaminomethylene)-2-benzoxazoleacetate (9), respectively. Reaction of the enamines (7, 8 and 9) with diketene, acetic anhydride, propionic anhydride, and active methylene compounds such as ethyl cyanoacetate and malononitrile gave rise to the corresponding pyrido [2, 1-b] benzoazoles (10-19).View full abstractDownload PDF (564K) -
YOSHIYA YAMAHIRA, TETSUO NOGUCHI, TAKESHI NOGUCHI, HIROSHI TAKENAKA, T ...1979 Volume 27 Issue 5 Pages 1190-1198
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe drug absorption characteristics of a lipid-containing oral dosage form were studied in human subjects and rats. Diazepam was employed as a model drug and medium-chain triglyceride (MCT) was used as a model lipid. When administered orally to four human subjects, there was no significant difference between diazepam soft capsules and tablets in the average plasma levels of the drug, due to a large intersubject variation. However, when administered to an individual subject repeatedly, the soft capsules showed the tendency of faster drug absorption and superior reproducibility in the plasma level-time curve, suggesting a more uniform drug absorption rate compared with the tablets. The mechanism of this effect was further investigated in the rat model dosing a small amount (2μl/rat) of MCT solution or aqueous suspension. After oral administration, the retention of diazepam in the small intestine was quite small compared with that in the stomach, suggesting the importance of the gastric disappearance rate in drug absorption from these preparations. The gastric drug disappearance rate of MCT solution was faster and significantly less variable than that of the aqueous suspension, which was considered to be the main cause of the more uniform drug absorption rate of the oral diazepam-MCT preparations. It is suggested that diazepam, though it is a weak base, was emptied from the stomach mostly while retained in the lipid, and thus was affected by the movement of MCT in the GI tract.View full abstractDownload PDF (896K) -
MAKOTO UCHINO, KUNIO SUZUKI, MINORU SEKIYA1979 Volume 27 Issue 5 Pages 1199-1206
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCleavage of the carbon-sulfur bond of sulfoxide was effected, when a phthalimidomethyl moiety is linked to the sulfur of sulfoxide, by the action of sulfuryl chloride, molecular chlorine or thionyl chloride, affording an organic sulfinyl chloride or sulfenyl chloride. In the presence of alcohol, chlorine also gave the sulfonyl chloride. The preparation of organic sulfinyl chlorides was extensively examined to investigate the generality of these reactions.View full abstractDownload PDF (637K) -
KAZUO KUBO, NORIKI ITO, YASUO ISOMURA, ISAO SOZU, HIROSHIGE HOMMA, MAS ...1979 Volume 27 Issue 5 Pages 1207-1213
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt has been found that Smiles rearrangement leading to N-p-chlorophenyl-6-β-hydroxyethylamino-4-phenyl-2 (1H)-pyridone (II) took place when 6-β-aminoethoxy-N-p-chlorophenyl-4-phenyl-2 (1H)-pyridone (III) was heated in acetic acid, and that the reaction of an N-substituted 6-chloro-4-phenyl-2 (1H)-pyridone (I) with ethylenediamine, 2-amino-ethanethiol or o-aminothiophenol gives condensed heterocyclic pyridones such as imidazopyridone (IV), thiazolopyridone (X) or benzothiazolopyridone (XV). This reaction is considered to proceed by ring transformation of an intermediate of the Smiles rearrangement. Some of these pyridone derivatives showed strong biological activities as analgesic and antiinflammatory agents.View full abstractDownload PDF (720K) -
ETSUKO SUZUKI, KENICHI SHIROTANI, YASUYUKI TSUDA, KEIJI SEKIGUCHI1979 Volume 27 Issue 5 Pages 1214-1222
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe size reduction of solid drugs was attempted utilizing the freeze-drying of a two-component system comprising a solute and a solvent. It was found that the concentration of the drug to be frozen greatly influenced the average particle size of the resulting powder. The component of a system which forms a hydrate or a solvate produced more finely divided particles than did that of a simple eutectic system. This can be attributed to the effect of the peritectic reaction in the process. As the griseofulvin and benzene system gives a phase diagram with an incongruent melting point and forms a 1 : 2 solvate, the average particle size of the freeze-dried powder could be reduced to the submicron level. On the addition of surfactants to this system, micronized particles were obtained and the dissolution rate of griseofulvin was improved considerably.View full abstractDownload PDF (1199K) -
HITOSHI SEKIKAWA, MASAHIRO NAKANO, TAKAICHI ARITA1979 Volume 27 Issue 5 Pages 1223-1230
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCoprecipitates of sulfamethizole-polyvinylpyrrolidone (PVP) and sulfisoxazole-PVP were prepared at various ratios. The dissolution rates of the drugs in the coprecipitates were greater when the ratio of drug to PVP was smaller. The dissolution rate of sulfamethizole in the coprecipitate was greater when PVP of smaller molecular weight was used. Dissolution patterns were different for sulfamethizole-PVP coprecipitate and sulfisoxazole-PVP coprecipitate ; recrystallization of the drug was observed following the dissolution of sulfisoxazole-PVP coprecipitate, whereas no recrystallization was found in the dissolution of sulfamethizole-PVP coprecipitate. A new dissolution model for coprecipitate is proposed.View full abstractDownload PDF (1897K) -
KATSUMI TAKATA, OSAMU FUJISHITA, SHIGEYOSHI HOKAMA1979 Volume 27 Issue 5 Pages 1231-1236
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSince prone water surfaces of faucet terminals are liable to suffer contamination due to airborne microbes, development of a microbial barrier faucet is necessary. A new test method was developed to investigate faucet performance. The equipment could jet 7.8×107 microbes per 1 g of Biofermin, which was selected as a suitable contaminant, as calculated on the basis of colony formation.View full abstractDownload PDF (691K) -
SATORU IKENOYA, KOICHI ABE, TOSHIRO TSUDA, YOSHIAKI YAMANO, OSAMU HIRO ...1979 Volume 27 Issue 5 Pages 1237-1244
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn electrochemical detector combined with high-performance liquid chromatography (HPLC-ECD) was applied to the analysis of tocopherols (TP), ubiquinones (UQ) and phylloquinone (PQ). n-Hexane extracts of these substances from blood were injected into a reversed-phase column (Nucleosil C-18). The minimum detection limits were 50, 150-200 and 100 pg for TP, UQ and PQ, respectively. Blood levels of these substances were in good agreement with those obtained by other methods. The HPLC-ECD method is a simple, sensitive and relatively rapid method, and should be useful for the determination of α-tocopherol, ubiquinone-10 and PQ in biological materials.View full abstractDownload PDF (776K) -
KUNIYOSHI TANAKA, AI NAKANISHI, KIMI MORIOKA, HIROMITSU KOJIMA, NARUMI ...1979 Volume 27 Issue 5 Pages 1245-1251
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSchiff bases (3, 4) were obtained by condensation of D-threo-2-amino-1-(4-nitrophenyl)-1, 3-propanediol (2) with salicylaldehyde and acetylacetone. Copper (II) chelates (5 and 6) were synthesized from 3 and 4, respectively, and their chemical structures were determined by elemental analysis, molecular weight measurement, and infrared and nuclear magnetic resonance spectroscopies. From the temperature dependence of their magnetic susceptibilities, 5, 6 and the phenylcarbamate (7) derived from 5 were inferred to be tetramers having cubane-type structures. The phenylcarbamate (9) derived from 6 was presumed to have a dimeric structure.View full abstractDownload PDF (732K) -
MUNEHISA ARISAWA, MASAKO FUKUTA, MINEO SHIMIZU, NAOKATA MORITA1979 Volume 27 Issue 5 Pages 1252-1254
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new flavone glycosides, comanthoside A (I), C24H24O12, mp 252-255°, and comanthoside B (II), C23H22O12, mp 209-210°, have been isolated from fresh leaves of Comanthosphace japonica S. MOORE (Labiatae). The structures of I and II have been determined as 5, 7-dihydroxy-6, 4'-dimethoxyflavone-7-O-β-D-glucuronic acid methyl ester and -7-O-β-D-glucuronide, respectively. Compounds I and II were also detected in C. stellipila S.M. by PPC and TLC.View full abstractDownload PDF (487K) -
MASATAKA ICHIKAWA, SHUICHI NABEYA, KEIJI MURAOKA, TAKUZO HISANO1979 Volume 27 Issue 5 Pages 1255-1264
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Arylbenzimidazole and 5-substituted derivatives were synthesized by condensation at p-substituted-o-phenylene nitrogens with 2- or 4-picoline in the presence of sulfur or with a carboxylic acid group in the presence of polyphosphoric acid. Imidazole cyclizations from N'-(o, m or p-substituted-phenyl) arylamidines were also investigated, using sodium hypochlorite to react with N-arylamidines at pH 3 to afford the corresponding imino chlorides in higher yields. The chlorides were heated with an excess of sodium carbonate in situ for cyclization to an imidazole. Their cyclizing efficiencies to benzimidazoles decreased in correlation with the order of pKa values due to the dissociation of the amidino site in alkaline aqueous buffers. The acidities of 7-substituted-2-arylbenzimidazoles formed by ring closure at the position ortho to the substituent on the aniline ring in N'-(m-substituted-phenyl) arylamidines and those of compounds formed by the ring closure of N'-(o-substituted-phenyl)-arylamidines fitted the Taft equation for which steric hindrances are negligible (log K/KCH3=ρ*σ*). On the other hand, the acidities of 5-substituted-2-arylbenzimidazoles formed by ring closure at the position para to the substituent on the aniline ring in N'-(m-substituted-phenyl) arylamidines, by ring closure of N'-(p-substituted-phenyl) arylamidines and by ring closure of p-substituted-o-phenylene diamines with a carboxylic acid group fitted the Hammett equation using σpara (p=1.3).View full abstractDownload PDF (990K) -
KEISUKE KITAMURA, TOMOKO KISHINO, KEIICHIRO HOZUMI1979 Volume 27 Issue 5 Pages 1264-1267
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe interaction of chlorpromazine-HCl with lecithin vesicles was investigated by carbon-13 nuclear magnetic resonance spectroscopy. Signal broadening of the drug induced by its addition to a vesicle-water (D2O) solution indicated the incorporation of the drug into the vesicle membrane. In the absence of the drug, two resolved signals arising from the carbonyl carbons of the external and internal layers of the vesicle were observed with 0.3 ppm shift difference, but the difference became almost undetectable on addition of the drug. This phenomenon suggests that the incorporated chlorpromazine was located near the carbonyl carbons in the vesicle membrane. Displacement of a trivalent cation from the membrane surface by chlorpromazine-HCl was confirmed by the observation that the upfield shift of exterior choline methyl carbons initially induced by the addition of a shift reagent, Yb3+, to the vesicle solution was canceled out when a sufficient amount of the drug was added to the sample solution.View full abstractDownload PDF (471K) -
FUMIO IINUMA, YAYOI HIRAGA, TOSHIO KINOSHITA, MITSUO WATANABE1979 Volume 27 Issue 5 Pages 1268-1271
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRapid, simple and sensitive detection of carbohydrates on thin layer plates was achieved by utilizing o-aminobenzenesulfonic acid-H3PO4 reagent, which was found to be stable in solution. This method facilitated the simultaneous fluorometric and colorimetric detection of carbohydrates with excellent sensitivity. This method was also applied for the determination of sugars using a scanning fluorophotometer.View full abstractDownload PDF (483K) -
HIDENOBU OHMORI, SHIRO NAKAI, MASAICHIRO MASUI1979 Volume 27 Issue 5 Pages 1271-1273
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSControlled potential electrolysis of anthracene at a glassy carbon anode in acetonitrile containing an excess of triethylphosphite and subsequent treatment of the product with sodium iodide resulted in the formation of 9, 10-bis (diethylphosphonyl)-9, 10-dihydroanthracene. Anodic phosphonylation was also performed on 4'-methoxybenzanilide to give 2'-diethylphosphonyl-4'-methoxybenzanilide.View full abstractDownload PDF (435K) -
MASAICHIRO MASUI, CHIHIRO UEDA, TAZUKO YASUOKA, HIDENOBU OHMORI1979 Volume 27 Issue 5 Pages 1274-1275
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThioureas accelerate the formation of N-nitrosodimethylamine more effectively than thiocyanate ion : among the compounds tested the order of effect was tetramethylthiourea>thiourea>N, N'-dimethylthiourea.View full abstractDownload PDF (360K) -
HEIHACHIRO TAGUCHI, TOHRU ENDO, ITIRO YOSIOKA, YOICHI IITAKA1979 Volume 27 Issue 5 Pages 1275-1276
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe configuration at C-8 position of patrinoside, isolated from Patrinia scabiosaefolia FISCHER (Valerianaceae) was revised as S configuration by X-ray crystallographic analysis. The absolute configurations of the other carbon atoms are also confirmed as 1S, 5S, 7S and 9S (1).View full abstractDownload PDF (329K) -
OTOHARU ISHIZAKA1979 Volume 27 Issue 5 Pages 1277-1279
Published: May 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDifferent from the hitherto developed direct electrolysis of water, this new method generates hydrogen gas from water easily, smoothly and immediately through an indirect processes, i.e. so-called double pre-catalytic decomposition consisting of two pre-catalytic processes. One of them consists of a metal-pile or alloyed catalyzer and the other of an ammoniac aqueous solution of metallic ammonium complex salts or hydroxides. These two pre-catalytic agents generate hydrogen gas from water by mutual contact reaction, producing aside ammine coordinate compounds from the ammonium complex salts or hydroxides in a redox-cyclic system introducing the environmental thermal energy from the outside atmosphere. These catalyzers are effectively useful for several days after once settled and only by supplying the decomposed amount of water from outside.View full abstractDownload PDF (439K)
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