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Volume 109, Issue 12
Displaying 1-10 of 10 articles from this issue
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Masataka IHARA1989 Volume 109 Issue 12 Pages 887-912
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFor the purpose of the construction of ring systems, three novel methodologies ; (1) sulfeno-cycloamination, (2) enamine annulation, and (3) intramolecular double Michael reaction, were developed. The usefulness of these methods has been proved by total syntheses of a number of natural products. Indolizidine alkaloids and β-lactam antibiotics were synthesized by application of the sulfeno-cycloamination. Total syntheses of Ipecac alkaloids, Corynanthe alkaloids and Camptotheca alkaloids were accomplished by exploitation of the enamine annulation. Diterpene, Aconitum alkaloid, angular triquinane sesquiterpenes, estrane type steroids, phenanthroindolizidine alkaloid and quinolizidine alkaloid were effectively synthesized by the intramolecular double Michael reaction as the key step.View full abstractDownload PDF (1759K) -
Kenji SAKAGAMI, Tadahiro WATANABE, Shunzo FUKATSU, Hajime NITTA, Minor ...1989 Volume 109 Issue 12 Pages 913-925
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS3-Alkylthio-7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino) acetamido] cephalosporins (6 and 7) and the 3-methoxy analogues (10) were prepared by coupling diphenylmethyl 7-amino-3-alkylthio-3-cephem-4-carboxylate (1 and 2) or diphenylmethyl 7-amino-3-methoxy-3-cephem-4-carboxylate with (Z)-2-(2-tritylaminothiazol-4-yl)-2-(O-substituted oxyimino) acetic acid (4), followed by deprotection and subjected to examination of antibacterial activities. The pivaloyloxymethyl esters (8 and 9) of the compounds (6 and 7) were also prepared and oral activities of these esters were compared with those of the parent compounds (6 and 7). The cephalosporins (6a-j and 7a-c) had potent and wide antibacterial spectra against Gram positive and Gram negative bacteria which were comparable to those of cefixime or cefteram. Among them, the cephalosporins (6f and 7c) and the pivaloyloxymethyl esters (8b and 9b) had good in vivo efficacy in mice against infections of Escherichia coli No. 29 and especially 8b showed high urinary recovery in mice.View full abstractDownload PDF (926K) -
Michinori KUBO, Tamae DOHI, Tsutomu ODANI, Hiroyuki TANAKA, Junichi IW ...1989 Volume 109 Issue 12 Pages 926-931
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe ethanol extract of Psoraleae Fructus (Psoralea corylifolia L.) was found to have cytotoxic activity against L929-cells in cell culture. The active compound was isolated by column chromatography on silica gel and identified as bakuchiol by means of spectral evidence. The cytotoxic activity of bakuchiol in cell culture was observed in short time and found to be unreversible. The mechanism of the cytotoxic activity was considered to be due to an injury of cell membrane from electron microscopic observation and hemolytic activity.View full abstractDownload PDF (1197K) -
Ichimaro YAMADA, Miwako KAWATA, Toshiyuki SHIBATA, Kenji OGAWA, Tetsuo ...1989 Volume 109 Issue 12 Pages 932-937
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSGround mixture of N, N-dimethylcarbamoylmethyl α, 2-dimethyl-5H-[1] benzopyrano-[2, 3-b] pyridine-7-acetate (1) with various pharmaceutical ingredients were prepared in order to investigate their dissolution behaviors and bioavailability. Taking into account the weakly basic property of 1, the dissolution rate was determined in the 2nd fluid (pH 6.8) of disintegration test, JP XI. Dissolution rates of the ground mixtures (1 : 1, w/w) of 1 with hydroxypropylcellulose-L (HPC-L), low substituted hydroxypropylcellulose (L-HPC) or lactose respectively, showed a significant increase compared with compound 1 alone. Three kinds of experimental fine granules were prepared ; type A : produced from ground mixture of 1, HPC-L, L-HPC and lactose ; type B : produced from physical mixture having the same composition as type A ; type C : produced 1, L-HPC and lactose. In these fine granules, only type A exhibited pH-independent dissolution profiles. Bioavailability study was carried out in beagle dogs whose gastric acidity was controlled in advance to low levels by administration of omeprazole. The test was conducted in a cross over design. Reflecting their dissolution characteristics, type A granules showed better bioavailability than the others. These results suggest that grinding is useful for the improvement of the dissolution property and bioavailability of 1, a weakly basic compound.View full abstractDownload PDF (634K) -
Koichiro KASE, Mayumi SHOSHIHARA, Yoshiko TSUDA, Eiko YOSHIZAWA, Takas ...1989 Volume 109 Issue 12 Pages 938-942
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn general, collection of serial blood samples from small experimental animals is difficult in terms of sampling site and operation technique. To overcome these problems, a simple reproducible method has been improved by the use of filter papers. Whole blood obtained by venipuncture from the ear vein of guinea-pig was spotted onto a filter paper. Isepamicin in the dried blood spot was extracted with 0.5 M Na2HPO4 buffer by incubation and determined by fluorescence polarization immunoassay. Linearity was established over the range of 5-150 μg/ml by using only 100 μl of whole blood. Consequently its accuracy and precision were good, with mean coefficient of variation of less than 5%. The method described here correlates well with a conventional sampling method and could be used for the pre-clinical study of isepamicin blood levels of individual guinea-pigs. This method is suitable for the simulataneous measurement of aminoglycoside antibiotics or physiological parameters after the administration of aminoglycoside antibiotics for the pharmacokinetics study.View full abstractDownload PDF (582K) -
Takuya KUKITA, Akemi YAMAGUCHI, Akihiko OKAMOTO, Masami NEMOTO, Hirosh ...1989 Volume 109 Issue 12 Pages 943-948
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe decrease of bromhexine HCl contents in granules and tablets was determined when the preparations were stored in polyethylene film package. Effects of temperature, contact area with film, excipients and moisture contents in the preparation on the remaining amount of bromhexin HCl were studied in order to investigate the interaction mechanism between bromhexine HCl and polyethylene film. It was observed that the decrease of bromhexine HCl was due to the sorption to the polyethylene film. The results indicated that the moisture contents of the dosage forms determined the rate of sorption predominantly, and that removal of adsorbed water from dosage forms was effective to prevent bromhexine HCl content decrease.View full abstractDownload PDF (625K) -
ChengMing WANG, Setsuko OHTA, Masato SHINODA1989 Volume 109 Issue 12 Pages 949-953
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe survival effect of mice irradiated with a lethal dose of X-ray was studied by use of 60 kinds of Chinese traditional medicines. Methanol extracts of these medicines were prepared, and then each extract injected intraperitoneally into male mice before or after whole-body irradiation. As a result of these studies, the survival effects with Ogi-kentyu-to, Simotu-to, Sessyoin, Zokumei-to and Boi-ogi-to were observed by intraperitoneal injection before irradiation. Of these effective methanol extracts, only Zokumei-to was shown to have a significant survival effect by intraperitoneal injection after irradiation.View full abstractDownload PDF (594K) -
Hiroshi TOMISAWA, Hiroshi HONGO, Hiroto NAKANO, Hisao MATSUZAKI1989 Volume 109 Issue 12 Pages 954-956
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe Diels-Alder reactions of 2-dicyanomethylene-1, 2-dihydro-1-methylpyridine (Ia), 1-methyl-2 (1H)-pyridone (IIa) and their monomethyl derivatives (Ib-e and IIc, e) with N-phenylmaleimide (IIIb) were studied in connection with the aromaticity of the dienes. The yields of adducts (IVa-e and Va, c, e) are well correlated with the corresponding Homo-Lumo interaction energy (ΔE) of the diene and the dienophile calculated by using CNDO/2 method. The reactivity of Ia as a diene is somewhat lower than that of IIa reflecting the fact that the aromaticity of the former exceeds that of the latter.View full abstractDownload PDF (373K) -
Kenji SAKAGAMI, Mika SAKAI, Tomohiro KASHI, Toshiyasu ISHIMARU1989 Volume 109 Issue 12 Pages 957-961
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSynthesis and oral activity of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)-acetamido]-3-(1, 2, 3-triazol-1-yl) methyl-3-cephem-4-carboxylic acid and its related compounds were described. 3-(1, 2, 3-Triazol-1-yl) methylcephalosporins have been prepared by the direct cycloaddition of acetylene to 3-azidomethylcephalosporins, which were obtained by nucleophilic substitution of 3-chloromethylcephalosporins with sodium azide in N, N-dimethylformamide. The cephalosporins (8a-c) had potent and wide antibacterial spectra against gram positive and gram negative bacteria which were comparable to those of cefixime or cefteram. Urinary recovery of 9a and 9b, pivaloyloxymethyl esters of 8a and 8b, were 9.2% and 3.5%, respectively, through oral administration in mice, exhibiting lower rate than that of cefteram pivoxyl (28%).View full abstractDownload PDF (594K) -
Junichi IWAMURA, Tamae DOHI, Hiroyuki TANAKA, Tsutomu ODANI, Michinori ...1989 Volume 109 Issue 12 Pages 962-965
Published: December 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBakuchiol is a major component of Corylifoliae Fructus (Psoralea corylifolia L.) and has been clarified to have cytotoxic activity. The chemical structure-cytotoxic activity relationship of bakuchiol was investigated by means of cytotoxic activity of synthesized analogues of bakuchiol and phenol. It was proved that an alkyl group was necessary for cytotoxic activity. But the double bonds in the unsaturated hydro-carbon group exerted but little influence on the cytotoxic activity. The cytotoxic activity of bakuchiol was the strongest as compared with that of the analogues examined.View full abstractDownload PDF (498K)
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