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Volume 42, Issue 8
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Gwenola BURGOT, Jean-Louis BURGOT1994 Volume 42 Issue 8 Pages 1553-1555
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe water/n-octanol partitioning thermodynamic parameters of some local anaesthesic agents are determined through a calorimetric estimation of the enthalpies of transfer. Partitionings are entropy-driven. Although no single mechanism of transfer can be ascribed, the mechanisms seem identical for each subfamily of the same kind of structure.View full abstractDownload PDF (477K) -
Zenei TAIRA, Mitsuhiro MATSUMOTO, Shiro ISHIDA, Tsutomu ICHIKAWA, Yoko ...1994 Volume 42 Issue 8 Pages 1556-1561
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe aggregation of DNA caused by coralyne was studied by spectroscopic, viscosity and electric birefringence measurements. Aggregation was markedly enhanced over a narrow range of coralyne to DNA phosphate ratio and then followed by precipitation. The electric birefringence measurements indicated that the ratio at the maximal aggregation varied depending on the concentration of coralyne, finally reaching 1 : 1 at higher concentrations. The particles (type I) for such enhanced aggregation were estimated to be prolate ellipsoids 1700-4000 Å in length with a diameter of 1400-4000 Å. At higher coralyne concentrations, another particle (type II) was formed which was a thick rod-like particle 1700-4000 Å in length with a diameter of 120-210 Å. These dimensions indicate that type I and II particles consist respectively of several tens of thousands and some hundreds of molecules of DNA.On the other hand, berberine did not produce such a marked aggregation of DNA, and the result was a thick rod-like particle 1700-4000 Å in length with a diameter of 300-1000 Å. The enhancement by coralyne and berberine is discussed in terms of intermolecular interactions.View full abstractDownload PDF (805K) -
Kazuho HARADA, Eisuke KAJI, Kiyobumi TAKAHASHI, Shonosuke ZEN1994 Volume 42 Issue 8 Pages 1562-1566
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Aryl-2-isoxazoline 2-oxides (1) were converted to methyl α-hydroxy-3-methoxycarbonyl-4H-1, 2-benzoxazine-4-acetates (3) upon treatment with a Lewis acid such as titanium tetrachloride. The structure of 3 was confirmed by X-ray analysis. Tosylates of 3 were treated with triethylamine to yield (E)- and (Z)- isomers of olefins (5) with (E)-preference. Catalytic reduction of each isomer of 5 produced 5, 8a-disubstituted 1, 3, 3a, 8a-tetrahydro-2H-benzofuro[2, 3-b]pyrrol-2-ones (6) in moderate yields.View full abstractDownload PDF (777K) -
Shunsaku NOGUCHI, Ayumi FUJII, Koki HASHITANI, Takashi ISHIZU1994 Volume 42 Issue 8 Pages 1567-1570
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSteroid-17α-hydroxy-17-carboxylic acids (2) were allowed to react with carbodiimides (DCCI, DPCI, DTCI, EDCI) to afford 17-spiro-5'-[2'-imino-4'-oxazolidinones] (3-5, 11), 17-spiro-5'-[2', 4'-oxazolidinediones] (7-9)and N-acylureas (10), depending on the reaction conditions. The reaction in acetonitrile in the presence of CuCl2 gave 3-5, while that in N, N-dimethylformamide gave 7-9. The reaction with DTCI under basic conditions afforded 10 along with 9.View full abstractDownload PDF (749K) -
Ryousuke TOUYAMA, Kenichiro INOUE, Yoshio TAKEDA, Masahiko YATSUZUKA, ...1994 Volume 42 Issue 8 Pages 1571-1578
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe mechanisms of the formation of brownish-red pigments having a 2-methyl-4-carbomethoxy-2-pyrindine nucleus as a basic skeleton by reaction of genipin with methylamine under an atmosphere of inert gas are discussed based on the isolation of 5, 6-dihydro-2-methyl-4-carbomethoxy-8-hydroxymethyl-2-pyrindine as a precursor and on comparisons of the results obtained from the reactions of genipin congeners and methylamine. The origin of the extra methyl group at C-6 in the structures of some of the brownish-red pigments was clarified to be the carbon atom of the hydroxymethyl group at C-8 of genipin by using deuterium-labelled genipin.View full abstractDownload PDF (920K) -
Toshihisa OGAWA, Katsuo HATAYAMA, Hiroshi MAEDA, Yasuyuki KITA1994 Volume 42 Issue 8 Pages 1579-1589
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeveral 3-(2-cyanoethyl)-1, 4-dihydropyridine carboxylates (16) were prepared in moderate to good yields by means of the Hantzsch reaction. Treatment of these carboxylates with a weak base such as sodium sulfide or tetrabutylammonium fluoride at room temperature afforded smoothly the corresponding 1, 4-dihydropyridine monocarboxylic acids (18) in good yields. The monocarboxylic acids 18n and 18o were esterified with 2-nitrooxypropanol or N-(2-hydroxyethyl)nicotinamide p-toluenesulfonic acid salt to afford the selective coronary vasodilators CD-349 (5) and CD-832 (6), respectively.View full abstractDownload PDF (1112K) -
Machiko ONO, Reiko TODOROKI, Yasuo YAMAMOTO, Hiroyuki AKITA1994 Volume 42 Issue 8 Pages 1590-1595
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactivity of methyl 4, 5-epoxy-(2E)-pentenoate (2) toward various aromatic nucleophiles in the presence of boron trifluoride etherate was examined. When benzene derivatives possessing an electron-donating substituent were employed, meta-substituted benzenes attacked only the 4-position of 2, while ortho- or para-substituted benzenes simultaneously attacked the 4- and 2-positions of 2.View full abstractDownload PDF (891K) -
Kazuyoshi OHASHI, Hiromi KOJIMA, Tatsuya TANIKAWA, Yasuaki OKUMURA, Ka ...1994 Volume 42 Issue 8 Pages 1596-1600
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new quinovic acid glycosides, named gongganosides A (1), B (2), and C (3), were isolated from the bark of Bhesa paniculata (Celastraceae), an Indonesian medicinal plant collected in Sumatra Island. The chemical structures have been elucidated on the basis of chemical and physicochemical evidence as quinovic acid 3-O-β-D-xylopyranosyl(1→3)-α-L-rhamnopyranoside for 1, 28-O-β-D-glucopyranosylquinovic acid 3-O-α-L-rhamnopyranoside for 2, and 28-O-β-D-glucopyranosyl-quinovic acid 3-O-β-D-xylopyranosyl(1→3)-α-L-rhamnopyranoside for 3.View full abstractDownload PDF (777K) -
Masahisa YAMAGUCHI, Takaki KOGA, Kenshi KAMEI, Michitaka AKIMA, Toshio ...1994 Volume 42 Issue 8 Pages 1601-1604
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis and pharmacological evaluation of novel 4-[2-(5-ethyl-2-thienyl)]-2-[2-(1-imidazolyl)ethyl]-1(2H)-phthalazinones are described. The phenyl moiety of the phthalazione skeleton was found to play an important role in both thromboxane A2 synthetase-inhibitory and bronchodilatory activities.View full abstractDownload PDF (628K) -
Abdellah ALSAIDI, Samir AL SHARGAPI, Patrick DALLEMAGNE, Franck CARREI ...1994 Volume 42 Issue 8 Pages 1605-1608
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of some new hydroxyaminocyclopenta[c]thiophenones was achieved via halogenation reaction, then formation and finally cleavage of an aziridino ring. The in vitro cytotoxic activity of these compounds was evaluated against L1210 leukemia. The importance of the ketohydroxyethylamino sequence for their activities is discussed.View full abstractDownload PDF (572K) -
Toshimi SEKI, Takayuki TAKEZAKI, Rikio OHUCHI, Hiroshi OHUYABU, Tsutom ...1994 Volume 42 Issue 8 Pages 1609-1616
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of hydrazinopyridazine derivatives combined with a β-blocking side chain were synthesized. When they were given intravenously to anesthetized rats, some of them exhibited both hypotensive and β-blocking activities. Their structure-activity relationships for hypotensive and β-blocking activities are discussed. Compound 11c had the best profile and was selected for further study.View full abstractDownload PDF (1020K) -
Eric NICOLAI, Gerard CURE, Joel GOYARD, Maud KIRCHNER, Jean-Marie TEUL ...1994 Volume 42 Issue 8 Pages 1617-1630
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis and pharmacological activity of new nonpeptide angiotensin II (AII) receptor antagonists are presented. These 5-O-substituted and 5-C-substituted 3-alkylpyrazole derivatives represent a new series of antagonists and have led to to the discovery of compounds with potent oral antihypertensive activity in a renal artery-ligated rat model. In vitro, they displayed a high affinity for rat adrenal AII receptors. In vivo structure-activity relationship study has shown the importance of the 4-[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl moiety for oral activity and the critical role of alkyl substituents at the 1- or 2-position. In the case of oral administration, 5-C derivatives were found to be, on the whole, more potent than 5-O derivatives. UP 221-78, 5-hydroxymethyl-3-n-propyl-1-(2, 2, 2-trifluoroethyl)-4-[[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl]-1H-pyrazole (79), displayed equivalent antihypertensive activity to the well known antagonist Losartan at 3 mg/kg p.o. in renal artery-ligated rats, with maximal decreases in mean arterial pressure of 60 and 63 mmHg for Losartan and UP 221-78, respectively.View full abstractDownload PDF (1638K) -
Hiroaki KOMATSU, Kimihiko YOSHII, Satoshi OKADA1994 Volume 42 Issue 8 Pages 1631-1635
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWater-content data for various drugs, estimated on the basis of weight decrease in a loss on drying (LOD) test or determined by the Karl-Fisher method (KF), were compared with values obtained with thermogravimetry (TG). TG/mass spectroscopy was also utilized for identification of volatile materials during the weight-loss process. The results suggest that the TG method can be applied to the determination of water content in drugs if their volatile contaminant is only water or the major volatile constituent is water, and that TG can be used as a substitute for the LOD test in cases, where expense or some other factor restrict the available sample size of a drug. It was further indicated that TG can be utilized for some drugs to which the KF method cannot be applied due to their insolubility in KF reagents.View full abstractDownload PDF (746K) -
Akio HASHIMOTO, Kazuya YAMASAKI, Yoshio KOKUSENYA, Takaaki MIYAMOTO, T ...1994 Volume 42 Issue 8 Pages 1636-1641
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe contents of free amino acids (FAA) and total amino acids (TAA; including peptide and protein forms) in 10 animal drugs were determined using precolumn-derivatization high performance liquid chromatography (HPLC). The results showed that the FAA and TAA content was characteristic for a particular animal crude drug. For example, Bezoar Bovis contained much more taurine relative to the FAA and TAA content compared with other crude drugs, and kokurozin contained much more TAA and much less secondary amino acids relative to TAA compared with koukuzin. FAA and TAA were proved to be "signal" constituents for the evaluation of animal crude drugs.View full abstractDownload PDF (748K) -
Atsushi WATANABE, Takehisa HANAWA, Masayasu SUGIHARA, Keiji YAMAMOTO1994 Volume 42 Issue 8 Pages 1642-1645
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUtilization of the solid mass containing phenytoin, sodium caseinate and microcrystalline cellulose (MCC) as a new dosage form for the elderly was studied. The solid mass was prepared by treatment of the powder mixture with high pressure steam at 115°C for 10 min. The stability of phenytoin in the solid mass was confirmed by infrared spectroscopy and high performance liquid chromatography. The extent of swelling of the solid mass containing phenytoin was investigated by water absorption test and gel strength test, and the swelling property was almost independent of the presence of phenytoin. The release profile of phenytoin from the solid mass was determined under various conditions, and was found to be influenced by the extent of swelling and the swollen state. It was observed that the protein adsorption to the phenytoin crystal surface and the addition of digestive enzyme also affected the release profile. In water, the solid mass prepared from a ground mixture of phenytoin and MCC showed remarkable improvement of release profile of phenytoin.View full abstractDownload PDF (625K) -
Yasutomi KATO, Hisakazu SUNADA, Yorinobu YONEZAWA, Ryuzo ISHINO1994 Volume 42 Issue 8 Pages 1646-1650
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to elucidate the influence of the particle size of water-soluble ingredients in a wax matrix and the solubility of drugs on the drug dissolution rate from a dosage form, reservoir devices were prepared from a wax matrix layer consisting of hydrogenated caster oil (HCO) and lactose, a drug reservoir and a water non-permeable layer of HCO, and dissolution tests were then carried out. Drug permeability and water penetrability of the wax matrix layer were affected by the particle size of lactose incorporated into the wax matrix layer. Drug permeability and water penetrability could be decreased by using smaller lactose particles. Tortuosity in the wax matrix layer after the dissolution of lactose could be increased inversely proportional to the particle size. Permeability of the wax matrix layer differed depending on the kinds of drugs forming the drug reservoir, which was attributed to differences in the solubility and viscosity of the drug saturated solution formed in the drug reservoir.View full abstractDownload PDF (1173K) -
Toshio YANAKI, Michihiro YAMAGUCHI1994 Volume 42 Issue 8 Pages 1651-1654
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dependence of the intrinsic viscosities ([η]) of seven well-characterized sodium hyaluronate (HA) samples in 0.2 M NaCl solution on shear rates (γ^^·) was investigated using four kinds of viscometers with γ^^· values ranging from 0.1 to 2000 s-1. Molecular weight distributions of these samples were checked by a gel permeation chromatograph connected to a low-angle laser light scattering photometer. The determination of [η] at zero shear rate ([η]0) for high molecular weight HA had to be made using low shear viscometers with γ^^·<250s-1, since [η] showed remarkable shear thinning behavior with increasing molecular weight. Double logarithmic plots of [η]0 vs. Mw (the weight-average molecular weight) for HA in 0.2 M NaCl solution gave a relation expressed by [η]0=1.99×10-4·M0.829w for Mw≥40×104, where [η]0 was written in dl/g unit. The shear thinning behavior of [η] of HA in the solvent was analyzed by the Rouse-Zimm bead-spring model proposed by Fixman. Consequently, the γ^^·-dependence of HA in 0.2 M NaCl solution could be well described by this model of large viscosity expansion factors, and suggested that an HA chain in the solvent is a fairly expanded random coil by excluded volume effects.View full abstractDownload PDF (620K) -
Tokujiro KITAGAWA, Junko ARITA, Atsuko NAGAHATA1994 Volume 42 Issue 8 Pages 1655-1657
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1, 1'-Oxalydiimidazole (7) reacts with formic acid (8) in acetonitrile at room temperature to give N-formyl-imidazole (5), which promptly undergoes aminolysis and alcoholysis to yield formamides (2) or formates (4).View full abstractDownload PDF (438K) -
Mitsuko MAEDA, Koichi KAWASAKI, Takeo TAGUCHI, Yoshiro KOBAYASHI, Yosh ...1994 Volume 42 Issue 8 Pages 1658-1662
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFluorinated analogs of Leu-enkephalin were synthesized by the solution method and the solid-phase method. The synthetic peptides were examined for opioid activities on mouse vas deferens and guinea pig ileum. Among the synthetic peptides, [D-Ala2, Leu(F3)(2R, 4S)5]enkephalin and [D-Ala2, Leu(F3)(2S, 4R)5]enkephalin exhibited potent opioid activity, and [Leu(F3)(2S, 4R)5]enkephalin exhibited high δ-receptor selectivity.View full abstractDownload PDF (806K) -
Kazuya YAMASAKI, Akio HASHIMOTO, Yoshio KOKUSENYA, Takaaki MIYAMOTO, T ...1994 Volume 42 Issue 8 Pages 1663-1665
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe antioxidative effects of methanol extracts of crude drugs were estimated by an electrochemical method because there are many electrochemically-active substances in natural antioxidants. Twelve kinds of crude drugs, which had been reported to exhibit strong activity in an antioxidative test based on the air oxidation of linoleic acid, were studied. The oxidative capacity calculated from voltammograms of their methanol extracts were compared and examined together with data on their radical scavenging effects. The results showed that the electrochemical behavior in most cases correlated with the radical scavenging effect. Crude drugs which had clear oxidative peaks below + 1.2 V and a large oxidative capacity were suggested to have strong radical scavenging effects. It was clear that substances oxidied at lower potentials had stronger radical scavenging effects than those oxidized at higher potentials. Therefore, this electrochemical method can be considered as a rapid and simple method for estimating the antioxidative effects as a radical scavenger.View full abstractDownload PDF (553K) -
Masashi TOMODA, Hiroko MIYAMOTO, Noriko SHIMIZU1994 Volume 42 Issue 8 Pages 1666-1668
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structural features of rehmannan SA, a polysaccharide with remarkable reticuloendothelial system-potentiating activity obtained from the root of Rehmannia glutinosa, were investigated by methylation analysis and periodate oxidation. Rehmannan SA is mainly made up of arabino-3, 6-galactan type structural units. Both rehmannan SA and rehmannan SB showed pronounced anti-complementary activity.View full abstractDownload PDF (496K) -
Kazuya KOSUGE, Katsuyoshi MITSUNAGA, Kazuo KOIKE, Taichi OHMOTO1994 Volume 42 Issue 8 Pages 1669-1671
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new phenolic glycoside, 3, 4, 5-trimethoxyphenol-1-(6-xylopyranosyl)glucopyranoside, was isolated together with twenty known compounds identified as koaburaside, 3, 4, 5-trimethoxyphenol, 5, 7-dihydroxychromone-7-neohesperidoside, naringin, neoeriocitrin, p-coumaric acid, vanillin, vanillic acid, coniferyl aldehyde, ferulic acid, trans-triacontyl-4-hydroxy-3-methoxycinnamate, p-methoxycinnamic acid, 2, 6-dimethoxybenzoquinone, 2-(1-hydroxyethyl)naphtho[2, 3-b]furan-4, 9-dione, 2-acetylnaphtho[2, 3-b]furan-4, 9-dione, 2-(1-hydroxyethyl)-6-methoxynaphtho[2, 3-b]furan-4, 9-dione, 2-acetyl-6-methoxynaphtho[2, 3-b]furan-4, 9-dione, specioside, jioglutin C and rehmaglutin D from the bark of Ailanthus integrifolia LAMK (Simaroubaceae).View full abstractDownload PDF (534K) -
Masato TAKAHASHI, Mayumi MOCHIZUKI, Kazumi WADA, Tomoka ITOH, Mihoko O ...1994 Volume 42 Issue 8 Pages 1672-1675
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA dissolution test was performed on a soft-gelatin capsule containing tocopherol nicotinate (TN) diluted with vegatable oil. The test methods were the paddle (PD) method described in the Japanese Pharmacopoeia (JP) and a rotating dialysis cell (RDC) method by which the sample is disintegrated inside a rotating cell covered with a filter and the contents are expelled from the cell into a solution outside.TN is practically insoluble. In the aqueous test solutions (pH 1.2 and 6.8), low dissolution rates were obtained by both the PD and RDC methods. However, we obtained a high dissolution rate by adding n-octanol, which has often been used for the measurement of drug partition coefficient, as a modification of the RDC method which has many factors controlling the drug dissolution. By examining the changes in the blood concentrations of TN after administration of the TN soft-gelatin capsule to humans, we established a relationship between the in vivo/in vitro findings.View full abstractDownload PDF (577K) -
Kazuharu SUMITA, Masayuki KOUMORI, Sachio OHNO1994 Volume 42 Issue 8 Pages 1676-1678
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMannich reaction of ketones using 1, 3-dioxolane instead of formaldehyde, paraformaldehyde, or 1, 3, 5-trioxane afforded the corresponding Mannich bases in high yields. Under the same conditions the aminomethylation of aromatics did not proceed but the intramolecular aminomethylation, like a Pictet-Spengler type reaction, proceeded smoothly.View full abstractDownload PDF (411K) -
Shin-ichi YAMADA, Sen-ichi NARITA1994 Volume 42 Issue 8 Pages 1679-1681
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour stereoisomers, (Rs, 9R)-(+)-5, (Ss, 9R)-(-)-5, (Ss, 9S)-(-)-5 and (Rs, 9S)-(+)-5, were prepared from optically active (R)-(+)-3 and (S)-(-)-3, and their absolute structures were unambiguously determined by X-ray crystallographic analysis of (Ss, 9R)-(-)-5. Epimerization of the carbon bearing the sulfinyl group of 5 could be carried out with NaOCH3. At the same time, it found that the stereochemistries of the sulfinyl group of (Rs, 9R)-(+)-5 and (Ss, 9S)-(-)-5 were spontaneously inverted in MeOH solution at room temperature.View full abstractDownload PDF (438K) -
Akira KAJI, Tomoki IWATA, Noriki KIRIYAMA, Shinya WAKUSAWA, Ken-ichi M ...1994 Volume 42 Issue 8 Pages 1682-1684
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new metabolites (1-4) were isolated from mycelium of Aspergillus terreus IFO 6123 producing asterriquinone (ARQ). The structures of 1 and 2 were shown to be 3, 6-bis[1-(1, 1-dimethyl-2-propenyl)-1H-indol-3-yl]-furo[3, 2-b]furan-2, 5-dione (asterridinone) and 2, 5-bis[1-(1, 1-dimethyl-2-propenyl)-1H-indol-3-yl]-3-acetoxy-6-hydroxy-2, 5-cyclohexadiene-1, 4-dione (ARQ monoacetate), respectively, by the chemical and spectral data. Compounds 3 and 4 were identified with known asterriquinone isomers, 2-[(1, 1-dimethyl-2-propenyl)-1H-indol-3-yl]-5-[2-(3-methyl-2-butenyl)-1H-indol-3-yl]-3, 6-dihydroxy-2, 5-cyclohexadiene-1, 4-dione (isoARQ) and 2, 5-bis[2-(3-methyl-2-butenyl)-1H-indol-3-yl]-3, 6-dihydroxy-2, 5-cyclohexadiene-1, 4-dione (neoARQ), respectively.View full abstractDownload PDF (430K) -
Hideaki SASAKI1994 Volume 42 Issue 8 Pages 1685-1687
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel DNA cleaving agent, N, N'-bis{2-[4-(3-aminopropylcarbamoyl)-2, 4'-bithiazol-2'-yl]ethyl}ethylenediamine (1), was synthesized. At 25μM concentration, a significant cleaving activity of 1 for plasmid DNA was observed only in the presence of Co(II). Scavengers of active oxygen species could not inhibit the DNA cleavage by 1.View full abstractDownload PDF (471K) -
Satoshi SHUTO, Takumi OBARA, Hiromichi ITOH, Yoshinori KOSUGI, Yasuyos ...1994 Volume 42 Issue 8 Pages 1688-1690
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Fluoro-and 2-chloroneplanocin A's (2 and 3) were synthesized as an adenosine deaminase resistant-equivalent of neplanoscin A, and evaluated for their antitumor and antiviral activities. Of these, 2 was completely resistant to adenosine deaminase and showed more significant antitumor and antiviral activities than neplanocin A.View full abstractDownload PDF (479K) -
Masayuki YOSHIKAWA, Tomohiko UEDA, Hisashi MATSUDA, Johji YAMAHARA, No ...1994 Volume 42 Issue 8 Pages 1691-1693
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new bioactive secoiridoid glucoside complexes named hydramacrosides A and B were isolated from the leaves of Hydrangea macrophylla SERINGE var. thunber gii MAKINO. The absolute stereostructures of hydramacrosides A and B were elucidated on the basis of chemical and physicochemical evidence which included the application of the 13C NMR glycosylation shift rule of 1, 1'-disaccharides and the modified Mosher's method. Hydramacrosides A and B exhibited inhibitory effect on the histamine release from rat mast cells induced by antigen-antibody reaction.View full abstractDownload PDF (529K) -
Tetsuya TAKEYA, Mitsuo NAKAGAWA, Akira OHGUCHI, Seisho TOBINAGA1994 Volume 42 Issue 8 Pages 1694-1696
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNon-enzimic and enzymic oxygenation reactions of (±)-dibenzocyclooctadiene lignan, (±)-deoxyschizandrin (1) using a simple model system for mono-oxygenases Fe(MeCN)62+-Ac2O-H2O2 and rat liver S9 mix were investigated in connection with mammalian and plant metabolisms of the corresponding lignans. The non-enzymic reaction of 1 gave the two phenol acetates 4a and 5a and a quinone 6, and the enzymic reaction of 1 afforded several compounds from which three compounds characterized as 7, 8, and 9 were isolated. The latter result has implications for biosynthesis of these lignans.View full abstractDownload PDF (438K) -
Ichiro YOKOE, Keiko MARUYAMA, Yoshiaki SUGITA, Tsutomu HARASHIDA, Yosh ...1994 Volume 42 Issue 8 Pages 1697-1699
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUtilizing an enaminoketone (1) as starting material, 3-substituted chromones were synthesized by the reactions of acid anhydrides derivatives under mild conditions.View full abstractDownload PDF (329K) -
Tatsuya MINAMI, Akemi NISHIMOTO, Yumi NAKAMURA, Miyoji HANAOKA1994 Volume 42 Issue 8 Pages 1700-1702
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCyclization of o-alkenylbenzoic acids in the presence of Pd catalyst and benzoquinone led to 3-substituted isocoumarins in high yield. The isocoumarins obtained were converted to isoquinolones by treatment with primary amines.View full abstractDownload PDF (413K) -
Jun OHWADA, Isao UMEDA, Hitomi ONTSUKA, Yuhko AOKI, Nobuo SHIMMA1994 Volume 42 Issue 8 Pages 1703-1705
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new antifungal substance, azoxybacilin (an unusual amino acid with an azoxy moiety) and its derivatives have been synthesized from Boc-L-Asp-OtBu utilizing the Moss procedure for the preparation of the azoxy moiety. The ester derivative, Ro 09-1824, showed more potent antifungal activity and a broader antifungal spectrum than azoxybacilin did.View full abstractDownload PDF (405K) -
Hajime KUBO, Shigeru OHMIYA, Kimio HIGASHIYAMA, Ken-ichi KAWAI, Kazuki ...1994 Volume 42 Issue 8 Pages 1706-1708
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe absolute structure of (+)-13β-hydroxymamanine (1), isolated from an alkaloidal component of Maackia amurensis (Leguminosae), has been established as (7R, 9S, 11R, 13R) by the X-ray analysis of its hydrobromide. The absolute stereochemistry of 1 is the same as that of the structure corresponding to an oxidative product derived from (-)-baptifoline (7R, 9R, 11R, 13R) coexisting in the same plant. It was strongly suggested that 1 might be an oxidative metabolite of (-)-baptifoline.View full abstractDownload PDF (383K) -
Yasufumi MARUYAMA, Muneaki KURIMURA, Kazuo ACHIWA1994 Volume 42 Issue 8 Pages 1709-1711
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMDP and lipopeptide analog conjugates inducing HIV-derived peptide-specific antibody without adding further macromolecular carriers or adjuvants were synthesized.View full abstractDownload PDF (383K) -
Shigetoshi KADOTA, Purusotam BASNET, Koji HASE, Tsuneo NAMBA1994 Volume 42 Issue 8 Pages 1712-1714
Published: August 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMatteuorienate A and B, two new C-methyl flavanone derivatives, were isolated from the Matteuccia orientalis (Hook.) Trev. (Aspidiaceae), and their structures were determined by the use of spectroscopic methods including 2D-NMR (1H-1H COSY, 1H-13C COSY and 1H-13C long-range COSY) experiments and chemical methods. Both the compounds were found to be very strong inhibitors of aldose reductase among the natural products.View full abstractDownload PDF (470K)
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