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Volume 112, Issue 10
Displaying 1-10 of 10 articles from this issue
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Yasushi YAMAZOE1992 Volume 112 Issue 10 Pages 679-692
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMechanisms of metabolic activation of carcinogenic chemicals, especially arylamines, are discussed together with characteristics of enzymes involved in the activation in the liver and extrahepatic tissues. In rodents, drug and carcinogen metabolizing activities often show clear age-and sex-related differences and also vary in diseased states. The current understanding of the roles of pituitary growth hormone and thyroid hormone on changes of hepatic drug metabolizing enzymes is shown in relation to the developmental changes and alteration in patho-physiological conditions.View full abstractDownload PDF (1358K) -
Ken KANEMATSU1992 Volume 112 Issue 10 Pages 693-711
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA new concept of cyclic conjugation as a modification of the Huckel rule has proven to be useful as a general method for predicting thermal stabilities and electronic properties of unsaturated cyclic organic molecules. We have been applying this concept to the design of reagents such as p-benzoquinone, polyquinones, and 1, 4-dithiins. Our efforts for the molecular design have relied extensively on the use of pericyclic reactions as pivotal steps in the total synthesis of polycyclic natural products incorporating fused heterocyclic subunits, targets that traditionally have provided fertile grounds for the development of new synthetic strategies. In order to obtain a quantitative understanding of the linkage between drug-bioreceptor complex formation, we have investigated the design and synthesis for the biologically active compounds (receptor probes) as follows : 1) the design and structure-activity relationship of a series of S-activated opioid agonist and antagonist ligands, 2) the design and synthesis of crowned morphine as the opioid receptor probes and 1, 4-benzoquinones as ionophore-dienophile combined systems, 3) synthesis of the base stacking and hydrogen-bonded nucleic acid base pair.View full abstractDownload PDF (1518K) -
Masahiro MAKINO, Mikihiko KUROSE, Yoshihiro SASADA, Hiroshi ZENDA, Shi ...1992 Volume 112 Issue 10 Pages 712-722
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSNew quaternary ammonium salts [N-alkyl-N-2-hydroxyethyl-N, N-dimethylammonium ethyl phosphate (21, 22), isopropyl phosphate (23), n-butyl phosphate (24) and N-alkyl-N-2-hydroxy-3-phenoxypropyl-N, N-dimethylammonium ethyl phosphate (25, 26), isopropyl phosphate (27), n-butyl phosphate (28) and bis(N-alkyl-N-2-hydroxy-3-phenoxypropyl-N, N-dimethylammonium) malate (29), fumalate (30), succinate (31), adipate (32) and N-alkyl-N-2-hydroxy-3-phenoxypropyl-N, N-dimethylammonium tartarate (33)] were synthesized by alkylation of the corresponding trialkylammonium salts with various epoxy compounds. The new quaternary ammonium salts showed much greater bactericidal activities and antirusting effects than those of benzalkonium chloride. They had also good compatibilities since no precipitate was observed if the solution of any anionic surface active agents were added to the solution of these new quaternary ammonium salts. This property is the same as that of amphoteric surface active agents.View full abstractDownload PDF (988K) -
Kazuo YAGO, Kazuo KAWADA, Tsuyoshi UCHIBORI, Shonosuke ZEN, Fumiya TOM ...1992 Volume 112 Issue 10 Pages 723-728
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA series of 3-O-alkyl and 3-O-haloalkyl-o-glucoses were prepared from 1, 2 : 5, 6-di-O-isopropylidene-α-D-glucofuranose and their antibacterial activities were evaluated. The compounds with C12 and C14-alkyl chains were the most effective in vitro antibacterial screening, among 3-O-alkyl and 3-O-haloalkyl derivatives. The 3-O-alkyl derivatives were more effective than 3-O-haloalkyl derivatives.View full abstractDownload PDF (552K) -
Shoetsu KONNO, Takeshi KOKUBO, Masaki AMANO, Nobuko YOSHIDA, Mataichi ...1992 Volume 112 Issue 10 Pages 729-741
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS5, 6-Diphenyl-, 3, 5-diphenyl-, and 3, 6-diphenyl-1, 2, 4-triazine (as-triazine) derivatives were evaluated for inhibitory activity towards arachidonic acid-induced aggregation of rabbit blood platelet in vitro. Among the isomers, 5, 6-diphenyl-as-triazine derivatives were active, therefore a phenyl substituent on the as-triazine ring at the 5-and 6-position was essential for the inhibitory activity. Thus, various 3-substituted 5, 6-diaryl-as-triazines were synthesized by the nucleophilic substitution reaction of 5, 6-diaryl-3-methylsulfonyl-as-triazines with O, N, C-nucleophiles. In the case of as-triazines having different aryl groups at the 5-and 6-positions, the compounds were prepared by the stepwise addition reaction of Grignard reagents with 3-methylthio-as-triazine. Among these compounds, ethyl 5-(4-methoxyphenyl)-6-phenyl-as-triazine-3-acetate (24a) and ethyl 5, 6-bis(4-methoxyphenyl)-as-triazine-3-acetate (24f) showed the most potent inhibitory activity, which was almost equal to the activity of anitrazafen.View full abstractDownload PDF (1095K) -
Masahiko OHSAKO, Yasuhiro MATSUMOTO1992 Volume 112 Issue 10 Pages 742-749
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe transport properties of benzoic acid and its eighteen derivatives such as o-, m-or p-hydroxybenzoic acid (o-, m-or p-HBA), aminobenzoic acid (o-, m-or p-ABA), toluic acid (o-, m-or p-TA), fluorobenzoic acid (o-, m-or p-FBA), chlorobenzoic acid (o-, m-or p-CBA) and bromobenzoic acid (o-, m-or p-BBA) through human erythrocyte membranes were examined. The drugs having a hydrophilic ortho-substituent and those having a hydrophobic meta-or para-substituent showed higher transport. The ratio of free drugs in erythrocytes, fuR, did not relate to the partition coefficient (P). However, fuM (the ratio of free drugs in the plasma) and Kp. (the ratio of partition between erythrocytes and plasma) related to the P : fuM=-0.3128×log P+0.9727 (R2=0.8722***), Kp=-0.2558×log P+0.8642 (R2=0.8413***). In p-nitrophenol-glycosides, the fuM and the Kp that were predicted from these equations were compatible with the experimental results. It was suggested from these results that the fuM and the Kp may be predictable from the P.View full abstractDownload PDF (760K) -
Kaori IMAMURA, Naohiro OISHI, Yasuhiko ISHIDA, Kenji OGAWA, Kazuhiko A ...1992 Volume 112 Issue 10 Pages 750-756
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPhysicochemical characteristics of crystalline water of (RS)-7-(2-amino-methylmorpholino)-1-cyclopropyl-6, 8-difluoro-1, 4-dihydro-4-oxo-3-quinoline-carboxylic acid were studied by thermal analyses and powder X-ray diffractmetry. The dihydrate of the compound was stable under ambient or humidified conditions. The dihydrate converted to a monohydrate on drying under mild conditions. The mono-and dihydrates transformed into α-type anhydrate at 110°C. These three kinds of crystals were convertible each other under appropriate conditions. At 165°C, the hydrates and the α-anhydrate converted to β-type anhydrate. The compressed effects on the crystalline waters were also discussed for the dihydrate by kinetic analyses.View full abstractDownload PDF (669K) -
Akihiko ITO, Yuka DOBASHI, Masayasu SUGIHARA1992 Volume 112 Issue 10 Pages 757-762
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe significance of the stationary time of punch in the process of compression on the dividing properties of scored tablets was investigated in several tablets prepared from lactose, corn starch, hydroxypropyl starch, synthetic aluminum silicate, microcrystalline cellulose or Perfiller<【○!R】>. The dividing strength of scored tablets was not affected by the stationary time of punch. The effect of the stationary time of punch on the coefficient of variation of divided tablet weight differed in the compacting characteristics and compaction profiles of powders. In case of tablets prepared from microcrystalline cellulose, the effect of stationary time of punch was not observed. However, in the other excipients, there existed a specific stationary time of punch to minimize the coefficient of variation of divided tablet weight. The time was different due to the change of compression pressure. The coefficient of variation of divided tablet weight showed minimum at the longer stationary time of punch when tablets were compressed at the low compression pressure, and the time showed a tendency to become short with the increase of compression pressure. These results suggested that the effect of the stationary time of punch on the coefficient of variation of divided tablet weight was concerned with the compaction structure of powders produced by the movement of punch in the process of compression.View full abstractDownload PDF (653K) -
Yoshihiro SAITO, Takatoshi SATO1992 Volume 112 Issue 10 Pages 763-767
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS -
Shoetsu KONNO, Mataichi SAGI, Kunio WADA, Futoshi SHIGA, Hiroshi YAMAN ...1992 Volume 112 Issue 10 Pages 768-772
Published: October 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA series of 6-alkylaminopyridazine-3-carboxylic acid derivatives was tested for dopamine β-hydroxylase inhibitory activity in vitro according to the method of Kruse et al. Methyl 6-alkylaminopyridazine-3-carboxylates (4) were synthesized through the reaction of methyl 6-chloropyridazine-3-carboxylate (1) with ammonia followed by the condensation with primary amines, and by the methanolysis of the resulting 6-alkylaminopyridazine-3-carboxa-mides (3) in methanol in the presence of boron trifluoride etherate. Among tested compounds, 6-benzylaminopyridazine-3-carboxylic acid was found to have the most potent inhibitory activity, which was in the same level of the activity of fusaric acid.View full abstractDownload PDF (533K)
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