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Volume 99, Issue 7
Displaying 1-15 of 15 articles from this issue
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SHINYA SHINOZAWA, YASUNORI ARAKI, TAKUZO ODA1979 Volume 99 Issue 7 Pages 693-698
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPositively charged, sonicated liposomes with [3H] prednisolone entrapped in them were administered to the rat hip muscle to examine its distribution in comparison with that after administration of free [3H] prednisolone. Plasma concentration of [3H] prednisolone in liposome-entrapped form was high for a long period of time, the values being 8 times after 30 min and 24 times after 24 hr compared to that in free form. The concentration of [3H] prednisolone in liposome-entrapped form in the liver, kidneys, and spleen was 4-10 times and, in the lung and pancreas, 8-10 times higher than that in free form after 30 min and 24 hr. In the adrenal, the concentration of liposome-entrapped prednisolone was lower than that in free form after 30 min and 1 hr, the former remained in the tissue, and the concentration was maintained at a high level after 24 hr, being about 28 times higher than that in free form. Even in the duodenum and large intestine, the liposome-entrapped form remained in the tissue for a long period of time. These facts suggested the usefulness of a small dose of intramuscular administration allowing the steroid to remain in the plasma and tissues for a long period of time.View full abstractDownload PDF (703K) -
SHINICHI NAGAI, NORIICHI ODA, ISOO ITO1979 Volume 99 Issue 7 Pages 699-704
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSOxidation of (4S, 7R)-2-amino-4, 7-methano-2H-indazole (2) with Pb (OAc)4 resulted in ring expansion to give (5S, 8R)-5, 8-methano-1, 2, 3-benzotriazine (5). Irradiation of 5 resulted in photolytic loss of nitrogen to give (1R, 3S)-ethynylcyclopentanecarbonitrile (6) by a radical reaction. Compound 2 was converted to (4S, 7R)-2-substituted-4, 7-methano-2H-indazoles (8, 10, 12, 13, 14 and 15) and pyridazino [1, 6-b] indazoles (9 and 11). Compound 5 showed prominent central nervous system stimulant activity in mice.View full abstractDownload PDF (744K) -
SHINICHI NAGAI, NORIICHI ODA, ISOO ITO1979 Volume 99 Issue 7 Pages 705-710
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS(1R, 4S)-3-Diazobornane-2-one was reacted with dimethyl acetylenedicarboxylate and methyl propiolate to give (4S, 7R)-4, 7-methano-8H-pyrazolo [1, 5-a] azepines (3a, b) (5R, 8S)-5, 8-methano-1H, 4H-cycloheptapyrazole (5) via spiropyrazole intermeadiate (6). The reaction from 6 to 3a, b and 5 is interpreted as a [1, 5] sigmatropic acyl rearrangement. Compound 3a was converted to (8R, 11S)-8, 11-methano-7H-benzo [3, 4] pyrazolo [1, 5-a]-azepine (12) and (8R, 11S)-8, 11-methano-7H-pyridazino [4', 5' : 4, 3] pyrazolo [1, 5-a] azepine (16). Treatment of 3a, b with sodium methoxide in methanol resulted in cleavage of amido linkage to yield (1R, 3S)-(pyrazol-5-yl) cyclopentanes (17a, b).View full abstractDownload PDF (737K) -
TOSHIKAZU TABATA, KAZUAKI YODEN, HIROSHI TAKEI, TOSHIHIRO IIO1979 Volume 99 Issue 7 Pages 711-716
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFluorescent substances were formed by the reaction of various amino compounds and malondialdehyde (MDA), the end product of lipid peroxidation. Reduction of these fluorescent substances with sodium borohydride resulted in disappearance of the fluorescence. Fluorescent substances were also obtained from the reaction of UV-irradiated phosphatidylethanolamine or methyl linolenate with 1-aminopentane, and the increase in fluorescent substances was accompanied by a decrease of thiobarbituric acid (TBA) reactants during the reaction. The resulting flnorescent substances were soluble in chloroform-methanol (2 : 1), and were not affected by treatment with sodium borohydride. On the other hand, fluorescent substances were not formed from conjugated diene compound, which is one of the primary compounds of lipid peroxidation. Lipofuscin-like fluorescent substances isolated from rat liver microsomes showed a similar characteristic to those derived from lipid peroxide and 1-aminopentane in vitro. These results suggested that lipofuscin-like fluorescent substances were not formed from MDA and amino compounds, but from TBA reactants, which were formed during the decomposition of conjugated diene compound to MDA in lipid peroxidation, by reaction with amino compounds.View full abstractDownload PDF (688K) -
ISAO UMEDA, HIROSHI ANZAI, ATSUSHI MURANO, HIROSHI NOGUCHI1979 Volume 99 Issue 7 Pages 717-722
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAn iodometric method was developed for the quantitative determination of new semisynthetic penicillins, sodium (2S, 5R, 6R)-6-[(R)-2-(4-hydroxy-1, 5-naphthyridine-3-carboxamido-2-phenyl acetamido]-3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate (PC-904, apalcillin sodium) and sodium (2S, 5R, 6R)-6-[(R)-2-(4-hydroxy-1, 5-naphthyridine-3-carboxamido)-2-(4-hydroxyphenyl) acetamido]-3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate (PC-462). These antibiotics were hydrolyzed to form corresponding penicilloic acids which consumed iodine. Accuracy and precision of this method depended upon the pH at which their penicilloic acids reacted with iodine, and pH 1.5±0.2 was found to be optimum. One mole of PC-904, PC-462, ampicillin or amoxycillin consumed 9.7 gramatom of iodine. The analytical results obtained by the iodometric method were in good agreement with those obtained by bioassay, including some samples partially decomposed.View full abstractDownload PDF (640K) -
KAZUO KIGASAWA, HIDEKI IIMURA, AKIRA TANIZAKI, SABURO SUGAHARA, KAZUO ...1979 Volume 99 Issue 7 Pages 723-729
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSDifference in the apparent density between the core and peripheral portion of a tablet was measured in order to observe the behavior of powder compressed into various shapes of tablets. In another experiment, double cylindrical tablets of various shapes were made by compressing colored powder in concentric circles to observe the movement of powder caused by compression in cross-sections of the double cylindrical tablets. Movement of a powder due to compression was not observed in tablets with a flat surface, whereas the movement of powder from the peripheral portion to the core was observed in tablets with a curved surface. Abnormal behavior of a powder, such as excessive movement toward the core, was observed in tablets with a flat surface on one side. A larger difference in the apparent density and movement of a powder caused by compression was observed in tablets with a smaller radius of curvature and thickness. These results supported the previous findings concerning the influence of tablet shape on the distribution of hardness inside the tablets.View full abstractDownload PDF (725K) -
TAKAKO HORI, KAISHU MOMONOI, YASUO KIBA, CHOSAKU YOSHIDA, HIROSHI SAKA ...1979 Volume 99 Issue 7 Pages 730-737
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS1-(2-Chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinylalkyl)-1-nitrosourea (Ia-r) were synthesized and their physico-chemical properties were examined. Along with an increase of the carbon number n between the nitrosourea moiety and the 2, 3-dioxopiperazine ring, the alkylating activity was reduced, the stability in aqueous solution at pH 7-8 was increased, and the NH proton of the nuclear magnetic resonance spectrum was shifted to a higher field. They were not related to the 4-substitutent R of the 2, 3-dioxopiperazine ring.View full abstractDownload PDF (723K) -
TAKAKO HORI, TAKASHI YASUDA, SHINJI MIYAHARA, SHOHACHI MURAKAMI, HISAT ...1979 Volume 99 Issue 7 Pages 738-744
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe structure-antitumor activity relationship of 1-(2-chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinylalkyl)-1-nitrosoureas I was investigated. The cytotoxocity against HeLa cells was most efective when the distribution coefficient of I in CHCl3-H2O (pH 7) was about 20. The antitumor activity against L1210 leukemia by intraperitoneal injection was related to the 4-substitutent R of the 2, 3-dioxopiperazine ring and the carbon number n between the nitrosourea moiety and the 2, 3-dioxopiperazine ring. Therefore, the more effective substituent R was H, Me, Et and the favorable carbon number n was 2-4. The acute toxicity in mice by intravenous injection was decreased along with an increase of the lipophilicity of I. Among the compounds of this series, 3, 5 and 11 were found to have a higher therapeutic ratio (LD50/ED60).View full abstractDownload PDF (585K) -
KOJI KURODA, TERUYOSHI YOKOYAMA, TSUNEO UMEDA, YOSHIAKI KITA, AKIRA KO ...1979 Volume 99 Issue 7 Pages 745-751
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPhysicochemical properties of the polymorphs and hydrate of 6-mercaptopurine were investigated. Its crystal habits were slightly changed and form I-TX was obtained by the addition of 6-thioxanthine and/or 2, 6-dithioxanthine and subsequent recrystallization. It was found that when Form I-TX was heated at 240°, this form transformed to Form III which was found to have a solubility about 6-7 times that of Form I. The mutual transition of 6-mercaptopurine polymorphs and hydrate under various conditions of heating and suspending in water was also studied. The transition temperature and the heat of transition between Form I-TX and Form II-TXhyd were determined to be 127°and 2.15 kcal/mol, respectively, by the solubility measurement. It was expected that if the transition of Form III could be suppressed, more bioavailable preparation of 6-mercaptopurine would be obtained.View full abstractDownload PDF (1161K) -
TETSUJI KAMETANI, KAZUO KIGASAWA, MINEHARU HIIRAGI, HARUHIDE ISHIMARU, ...1979 Volume 99 Issue 7 Pages 752-756
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSCondensation of trans-2-(3-hydroxyphenyl) cyclohexanol with various carbonyl compounds in the presence of acid gave 6-substituted hexahydro-6H-dibenzopyran derivatives. The antifungal activity of these compounds is under investigation.View full abstractDownload PDF (513K) -
YUKI NOGAMI, OSAMU FUTSUKAICHI, MICHITAKA OGAWA, TAMOTSU KOIZUMI1979 Volume 99 Issue 7 Pages 757-764
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAbsorption, distribution, excretion, and placental transfer of 14C-l-ST-2121 were studied by the tracer technique after its subcutaneous injection in male and female rats. 14C-l-ST-2121 was rapidly and almost quantitatively absorbed from the subcutaneous region. The radioactivity in blood reached the maximum level within 1 hr, and biphasic time course was observed. The radioactivity was rapidly distributed throughout the tissues. A high concentration of radioactivity was observed in the liver, kidneys, lung, hypophysis, Harderian gland, salivary gland, adrenal, and preputial gland. At 48 hr, a very low concentration was found in the tissues. In pregnant rats, a small amount of radioactivity passed through the placental barrier. The absorbed radioactivity was rapidly excreted in the bile and entered into enterohepatic circulation. Subsequent excretion of radioactivity was about 90% in urine, less than 7% in feces, about 40% in bile, and less than 1.5% in the expired air within 48 hr. Binding ratio of radioactivity to plasma protein was about 40% and transfer ratio of radioactivity to blood cell was about 30%.View full abstractDownload PDF (1495K) -
ISAO UMEDA, ATSUSHI MURANO1979 Volume 99 Issue 7 Pages 765-769
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSeparation and determination of new semisynthetic penicillins, sodium (2S, 5R, 6R)-6-[(R)-2-(4-hydroxy-1, 5-naphthyridine-3-carboxamido)-2-phenyl acetamido]-3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate (PC-904, apalcillin sodium) and sodium (2S, 5R, 6R)-6-[(R)-2-(4-hydroxy-1, 5-naphthyridine-3-carboxamido)-2-(4-hydroxyphenyl) acetamido]-3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate (PC-462), was carried out by high performance liquid chromatography (HPLC). PC-904 or PC-462 was separated from its penicilloic and penilloic acids under the following conditions : column, stainless steel (2.1 mm i.d.×1 m) packed with Zipax WAX ; column temperature, 40°; mobile phase, 0.01 M pH 3.4 citrate buffer at a flow rate of 0.7 ml/min, and determined by UV photometry at 254 nm. The analytical results obtained by HPLC were in good agreement with those obtained by the iodometric method previously reported, including some samples with were partially decomposed under drastic conditions.View full abstractDownload PDF (522K) -
ISAO UMEDA, HIROSHI ANZAI, ATSUSHI MURANO1979 Volume 99 Issue 7 Pages 770-774
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAnalytical methods were developed for the determination of a new antibacterial agent, 5, 8-dihydro-5-methoxy-8-oxo-2H-1, 3-dioxolo [4, 5-g] quinoline-7-carboxylic acid (miloxacin) by high performance liquid chromatography (HPLC) and ultraviolet spectrophotometry (UV). Miloxacin was separated from its impurities or degradation compounds by HPLC under the following condition : stainless steel column (2.1 mm i.d.×1 m) packed with strong anionic ion exchanger ; column temperature, 40°; mobile phase, pH 5.0 solution containing 0.01 M citrate buffer and 0.03 M sodium nitrate at the flow rate of 0.7 ml/min ; detector, a UV detector at the wavelength of 254 nm. Miloxacin could be determined with a relative standard deviation of 1% using picolinic acid as internal standard and its impurities were also determined at the same time. Moreover, miloxacin was dissolved in 1% sodium carbonate solution and determined by measuring the absorbance of the solution at the wavelength of 344 nm with a relative standard deviation of 0.3%. The impurities did not interfere with the determination of miloxacin and the results obtained by UV were in good agreement with those obtained by HPLC within experimental error, including some samples partially decomposed.View full abstractDownload PDF (528K) -
HISASHI ICHIBAGASE, YORISHIGE IMAMURA, AYAKA SUENAGA, TATSUYA YAMAGUCH ...1979 Volume 99 Issue 7 Pages 775-778
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSHypoglycemic activity of tolbutamide or chlorpropamide during continuous administration was found to be gradually enhanced by continuous administration of pyridinol carbamate in rabbits. In addition, it was suggested that the enhanced hypoglycemic activity resulted from the decreased renal excretion of these oral antidiabetic drugs by continuous administration of pyridinolcarbamate.View full abstractDownload PDF (477K) -
SHOJI TAKEMURA, HIROMI TERAUCHI, YASUYOSHI MIKI, KEIKO NAKANO, YOSHIHI ...1979 Volume 99 Issue 7 Pages 779-781
Published: July 25, 1979
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBenzhydryl derivatives of hydroxy- and amino-benzoic acids were synthesized and their biological activities were examined. Among them, 4-chloro-(2), 4-methyl-(4), and 4-methoxy-(5) benzhydrylsalicylic acids and 4-chloro-(7), and 4-methoxy-(10) benzhydryl anthranilic acids showed strong growth-inhibitory effects against Gram-positive bacteria. 4-(4-Methylbenzhydryl)-anthranilic acid (23) also inhibited the growth of Bacillus subtilis. Some of the salicylic and anthranilic acid derivatives were shown to be potent analgesics by the acetic acidstretching method.View full abstractDownload PDF (371K)
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