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Volume 43, Issue 3
Displaying 1-32 of 32 articles from this issue
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Katsuhiko NAKAMURA, Kazuya HAYASHI, Ikuo UEDA, Hideaki FUJIWARA1995 Volume 43 Issue 3 Pages 369-373
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPartition properties have been determined for 28 monosubstituted phenols in the sodium dodecylsulfate (SDS)/water system by micellar liquid chromtography (MLC), offering a useful and versatile method to estimate the hydrophobicity of compounds. The enthalpy and entropy terms of partition have also been determined from variable temperature experiments on MLC and are interpreted by such factors as molecular size and hydrogen-bond ability of the solute. The π constants (π, πH and πS) are determined from the experimental partition properties and applied to quantitative structure-activity relationships (QSAR) analysis, and their versatility supported.View full abstractDownload PDF (761K) -
Marie T. MOONEY, Shuhei DEGUCHI, Toshiji TADA, Mamoru FUJIOKA, Yoshihi ...1995 Volume 43 Issue 3 Pages 374-377
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCefdinir (CFDN) is an orally active, semisynthetic cephalosporin antibiotic and its structure is characterized by an oxyimino side chain which is able to form complexes with various metal ions. We observed that bioavailability of CFDN in dogs was reduced when it was co-administered with iron(II) salts. To assess possible effects of extraneous iron such as iron supplements on the bioavailability of CFDN, stability constants of the complexes formed between CFDN and iron(II) and iron(III) have been determined in aqueous solution by potentiometric and spectrophotometric titration methods. The stability constants were as follows : log β110=7.53, log β120=14.44, log β130=18.33 for the iron(II) complexes and log β110=10.43, log β120=20.40 and log β130=27.54 for the iron(III) complexes. Theoretical species distribution diagrams as a function of pH for solutions of metal (M) (0.1 mM) and ligand (L) (0.3 mM) showed that M1L1H0 and M1L2H0 existed as major species for the iron(II) system and M1L2H0 and M1L3H0 were main species for the iron(III) system under neutral conditions. From these results it is believed that complex formation in the digestive tract is involved in the reduction of the bioavailability of CFDN in dogs. In addition, spectrophotometric studies indicated that iron(II) coordinated to CFDN via the thiazole-ring and deprotonated oxime nitrogen atoms and iron(III) coordinated via the amide and deprotonated oxime oxygen atoms.View full abstractDownload PDF (630K) -
Tohru YASUZAWA, Ken'ichi MUROI, Michio ICHIMURA, Isami TAKAHASHI, Tats ...1995 Volume 43 Issue 3 Pages 378-391
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeven novel potent antitumor antibiotics, duocarmycins A (1), C1 (2), C2 (3), D (4), B1 (5), B2 (6) and SA (7), were isolated from three independently collected Streptomyces sp. The complete structures, including absolute stereochemistry, were determined by spectral and chemical studies of those duocarmycins and several derivatives. Duocarmycins A (1) and SA (7) possess a 1, 2, 7, 7a-tetrahydrocycloprop[1, 2-c]indol-4-one subunit, a common pharmacophore with that of CC-1065 (10) found from Streptomyces zelensis.View full abstractDownload PDF (1957K) -
Akira IIDA, Masaki SANEKATA, Shun-ichi WADA, Tetsuro FUJITA, Hiromi TA ...1995 Volume 43 Issue 3 Pages 392-397
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNew membrane-modifying peptides, trichorozing I-IV, have been isolated from conidia of the fungus Trichoderma harzianum. Their amino acid sequences were clearly determined by spectrometric methods and, furthermore, they were synthesized by the solution-phase method. Trichorozins are a family of the class of peptaibols and are composed of 11 residues including an amino alcohol. Trichorozins exhibited voltage-dependent ion channel-like activity in lipid bilayers.View full abstractDownload PDF (853K) -
Taisuke ITAYA, Shigeyuki SHIMIZU1995 Volume 43 Issue 3 Pages 398-402
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAmong N-protected and unprotected vinylglycines tested, N-(benzyloxycarbonyl)vinylglycine (1c) provided the highest yield of the coupling product 3c in the reaction with 1-iodo-4-methoxybenzene (2) in N, N-dimethylformamide in the presence of palladium acetate, sodium bicarbonate, and tetrabutylammonium chloride, whereas none of the desired product was obtained in the reaction with 4-methoxyphenyl trifluoromethanesulfonate (7). The stereoselectivity of the reaction was reversed by employing triethylamine instead of sodium bicarbonate to furnish (Z)-3c predominantly. In the presene of sodium bicarbonate, replacement of the solvent by water improved not only the chemical yield and stereoselectivity but also the optical purity : geometrically pure (E)-3c of 96% ee was formed in a good yield.View full abstractDownload PDF (859K) -
Jun'ichi KOBAYASHI, Kaori HONMA, Takuma SASAKI, Masashi TSUDA1995 Volume 43 Issue 3 Pages 403-407
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNine new bromotyrosine alkaloids, purealidins J-R (1-9), have been isolated from the Okinawan marine sponge Psammaplysilla purea and the structures were elucidated on the basis of spectroscopic data. A hydroxy group as C-1 of purealidins M-O (4-6) may be biosynthetically derived from ring-opening of a spirocyclohexadienyl-isoxazole unit of purealidin J (1), aerophobin-1 (10), and purealidin L (3), respectively. Purealidins N (5), P (7), and Q (8) were cytotoxic to tumor cell lines, while purealidins J (1), K (2), P (7), and Q (8) showed moderate inhibitory activity against epidermal growth factor (EGF) receptor kinase.View full abstractDownload PDF (778K) -
Tozo FUJII, Kazuo OGAWA, Taisuke ITAYA, Tadamasa DATE, Jin-ichiro INAG ...1995 Volume 43 Issue 3 Pages 408-413
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA full account is given of the first syntheses of 6-mercaptopurine 7-N-oxide (4) and 6-methylthiopurine 7-N-oxide (5). The synthesis of 4 followed a "phenacylamine route", which started from condensation of 4, 6-dichloro-5-nitropyrimidine (15) with N-(4-methoxybenzyl)phenacylamine to form the phenacylaminopyrimidine derivative (11) and proceeded through conversion into the mercapto derivative, intramolecular cyclization between the NO2 nitrogen atom and the phenacyl carbanion to give 6-mercapto-9-(4-methoxybenzyl)purine 7-N-oxide (12), and removal of the 4-methoxybenzyl group. S-Methylation of 12 and removal of the 4-methoxybenzyl group afforded 5. The location of the oxygen function in 4, 5, and 12 was confirmed by X-ray crystallographic analysis of 5·H2O, which was shown to exist in the N(7)-OH form (19). A UV spectroscopic approach suggested that the neutral species of 4 exists in HO as the N(7)-OH tautomer (21), whereas that of 5 exists as an equilibrated mixture of the N(7)-oxide (5) and the N(7)-OH (19) tautomers. In the in vitro bioassay of antileukemic activity against murine L5178Y cells, the N-oxides 4 and 12 were found to be weakly cytotoxic.View full abstractDownload PDF (1022K) -
Yoshitomo SUHARA, Kazuo ACHIWA1995 Volume 43 Issue 3 Pages 414-420
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-O-(α-D-Glucopyranosyl)-αHMJ (Glcα1, 4HMJ), 4-O-(α-mannopyranosyl)-αHMJ (Manα1, 4αHMJ), 4-O-(α-glucopyranosyl)-βHMJ (Glcα1, 4βHMJ), and 4-O-(α-mannopyranosyl)-βHMJ (Manα1, 4βHMJ) were synthesized as endomannosidase inhibitors which are potentially useful both for probing the pathways of N-linked glycoprotein processing and for the chemotherapy of some viral diseases.View full abstractDownload PDF (1004K) -
Shin-ichi YAMADA, Takao GOTO, Takaji YAMAGUCHI, Kazuyuki AIHIARA, Kent ...1995 Volume 43 Issue 3 Pages 421-431
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 2-[(cycloalka[b]pyridinyl)sulfinyl]-1H-benzimidazoles (11) was synthesized and tested for antisecretory activity against pentagastrin-induced gastric acid secretion in rats. A novel benzimidazole derivative containing a cyclohepta[b]pyridine moiety was found to be the most potent among the congeners, which included five- to eight-membered cycloalka[b]pyridine ring systems. Some 2-[(6, 7, 8, 9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl)sulfinyl]-1H-benzimidazole analogs (14) with various substituents on the aromatic rings showed superior properties to omeprazole (1) in biological examinations in vivo. A diastereoisomer, TY-11345 (28Ba), was selected as a promising agent for further evaluation.View full abstractDownload PDF (1583K) -
Akihiro TASAKA, Norikazu TAMURA, Yoshihiro MATSUSHITA, Tomoyuki KITAZA ...1995 Volume 43 Issue 3 Pages 432-440
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(2R, 3R)-3-Azolyl-2-(substituted phenyl)-1-(1H-1, 2, 4-triazol-1-yl)-2-butanols (III) were prepared from (2R, 3S)-3-methyl-2-(substituted phenyl)-2-(1H-1, 2, 4-triazol-1-yl)methyloxiranes (21a-f) by a ring-opening reaction with 1H-1, 2, 3-triazole and 1H-tetrazole and evaluated for antifungal activity against Candida albicans in vitro and in vivo. The optically active oxiranes (21a-f), which serve as the key synthetic intermediates, were synthesized from 1-[(2R)-2-(3, 4, 5, 6-tetrahydro-2H-pyran-2-yl)oxypropanoyl]morpholine (24) and substituted phenylmagnesium bromide (23) via six steps in a stereocontrolled manner. The 3-(1H-1, 2, 3, -triazol-1-yl)-(IIIa) and 3-(2H-2-tetrazolyl)-2-butanol (IIId) derivatives showed strong protective effects against candidosis in mice.View full abstractDownload PDF (1139K) -
Akihiro TASAKA, Noboru TSUCHIMORI, Tomoyuki KITAZAKI, Katsuhiko HIROE, ...1995 Volume 43 Issue 3 Pages 441-449
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe (2S, 3S)-, (2R, 3S)- and (2S, 3R)-stereoisomers of (2R, 3R)-3-azolyl-2-(substituted phenyl)-1-(1H-1, 2, 4-triazol-1-yl)-2-butanols [(2R, 3R)-1a-d] were prepared and evaluated for antifungal activity against Candida albicans in vitro and in vivo to clarify the relationships between stereochemistry and biological activities. The results revealed that the in vitro antifungal activity in each set of the four stereoisomers [(2R, 3R)-, (2S, 3S)-, (2R, 3S)- and (2S, 3R)-1a-d] definitely paralleled the in vivo antifungal activity against candidosis in mice, and the order of potency was (2R, 3R)»(2R, 3S)≥(2S, 3S)≥(2S, 3R).In addition, the four stereoisomers in each set were assessed for sterol biosynthesis-inhibitory activities in C. albicans and rat liver. The (2R, 3R)-isomer was found to exert a strong and selective inhibitory effect on the sterol synthesis in C. albicans as compared with that in rat liver.View full abstractDownload PDF (1210K) -
Ryuichi KIYAMA, Masahiro FUJI, Mariko HARA, Masafumi FUJIMOTO, Tomoji ...1995 Volume 43 Issue 3 Pages 450-460
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSStarting from recently reported nonpeptidic angiotensin II (AII) receptor antagonists, we have designed and prepared a new series of 6-arylimidazo[4, 5-c]pyridine derivatives. Variation of phenyl groups at the 4-, 6- or 7-position of imidazo[4, 5-c]pyridine showed that substitution at the 6-position resulted in receptor-binding activity almost as potent as that of DuP 753. This led to synthesis and evaluation of an extensive series of 6-aryl-imidazo[4, 5-c]pyridine derivatives. Some of them were 4-fold more potent in vitro than DuP 753, but only showed weak antihypertensive activity in vivo when given orally to rats.View full abstractDownload PDF (1434K) -
Hiroshi WADA, Yasufumi SHIMIZU, Nobutoshi TANAKA, Richard C. CAMBIE, J ...1995 Volume 43 Issue 3 Pages 461-465
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive new glycosides, 3, 4-dihydroxyphenethyl alcohol 4-O-caffeoyl-β-D-allopyranoside, (6S, 13S)-13-β-D-fucopyranosyloxy-6-{β-D-fucopyranosyl-(1→2)-[β-D-fucopyranosyl-(1→4)-α-L-rhamnopyranosyloxy]}-cleroda-3, 14-diene, (6S, 13S)-13-β-D-fucopyranosyloxy-6-{β-D-quinovopyranosyl-(1→2)-[β-D-fucopyranosyl-(1→4)-α-L-rhamnopyranosyloxy]}-cleroda-3, 14-diene, (6S, 13S)-13-α-L-arabinopyranosyloxy-6-{β-D-fucopyranosyl-(1→2)-[β-D-fucopyranosyl-(1→4)-α-L-rhamnopyranosyloxy]}-cleroda-3, 14-diene and (6S, 13S)-13-α-L-arabinopyranosyloxy-6-{β-D-quinovopyranosyl-(1→2)-[β-D-fucopyranosyl-(1→4)-α-L-rhamnopyranosyloxy]}-cleroda-3, 14-diene, were isolated, together with mangiferin and 6'-O-acetylmangiferin, from the fronds of a New Zealand fern, Trichomanes reniforme.View full abstractDownload PDF (792K) -
Toshio MIYASE, Hideki SAITOH, Ken-ichi SHIOKAWA, Akira UENO1995 Volume 43 Issue 3 Pages 466-472
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSix new oleanane-type triterpene saponins, called reiniosides A-F, were isolated from the roots of Polygala reinii FR. et SAV. and their structures were elucidated by spectroscopic and chemical means.View full abstractDownload PDF (763K) -
Tadashi MAKINO, Norimasa WADA, Nobuyuki KITAMORI1995 Volume 43 Issue 3 Pages 473-475
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn Onlator[○!R], a heat exchanger, was utilized as a continuous starch paste supplier for a fluidized-bed granulator. Ascorbic acid was used as a model drug substance and cornstarch as the binder. To control the temperature of cooking starch paste, modes of proportional control (P control) and proportional integral deviation (PID control) were used to distinguish their respective effects on the tablet properties. It was shown that the PID control caused less variation in the temperature of cooking starch paste and, in accordance with this, that variation in disintegration time for the resultant tablets was less. there was, however, little difference in tablet hardness between these two modes of control.View full abstractDownload PDF (517K) -
Masami MORITA, Toru HOSOKAMI, Tutomu KONNO, Koji KINUNO, Eiichi MAFUNE ...1995 Volume 43 Issue 3 Pages 476-482
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPreliminary preformulation studies of a 2-(3, 4-dimethoxyphenyl)ethylamine derivative were investigated. The hydrochloride form showed incompatibility with the excipients used for oral dosage forms. There were several crystal forms of the free base, namely, α-anhydrate, β-anhydrate, monohydrate, and trihydrate. The trihydrate form was unstable. The degree of crystallinity of the β-anhydrate form was difficult to control. The monohydrate form was difficult to manufacture with constant quality.The serum levels of the compounds in rats were almost related to the dissolution rates in the JP 1st disintegration medium from the discs. The serum level of α-anhydrate was the lowest. However, the dissolution rates from the formulations of α-anhydrate were improved. After oral administration of the improved formulation, the serum level of α-anhydrate in beagle dogs was almost triple that after the oral administration of the capsule of the hydrochloride form.View full abstractDownload PDF (1251K) -
Guojie XU, Hisakazu SUNADA1995 Volume 43 Issue 3 Pages 483-487
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSExamination was made of the release of indomethacin from hydroxypropylmethylcellulose (HPMC) matrices and the results were found to usually follow first order release kinetics. The release mechanism changed with formulation. HPMC content was the predominant controlling factor. As the HPMC content increased, drug release rate decreased, and the release mechanism gradually changed from Higuchi diffusion release to case II transport. Additives increased the release rate and enhanced Fickian diffusion. As drug content increased, release rate calculated from percent release data decreased while that calculated from mg release data increased. When indomethacin content was lower, drug release was diffusion controlled and when higher, non-Fickian transport of case II transport was apparent.Additive effects were also examined. Starch was found to most effectively maintain case II release. Complex additives containing starch were superior to any additive by itself.A multiple regression model was used to determine the relationship between response (release rate) and factors (content of HPMC and diluents), and on the basis of this model a formulation was established and found valid by agreement with data from the regression model.View full abstractDownload PDF (684K) -
Eijiro HORISAWA, Akio KOMURA, Kazumi DANJO, Akinobu OTSUKA1995 Volume 43 Issue 3 Pages 488-492
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of the physicochemical properties of binders on the strength of granules prepared by the wet method was investigated using hydrophobic and hydrophilic powders with various polymer binders. A crushing test of granules and the amount of fine granules generated during a sieving test were carried out in order to estimate the strength of the granules. In all the powder/binder systems, the surface polarities of both powders and binders, as well as the degree of polymerization of a binder, are important factors in determining the strength of granules. That is, binders and powders whose polarities are similar are capable of producing strong granules. In some systems, the strength of granules increased with the degree of polymerization of the polymer binders.View full abstractDownload PDF (726K) -
Ermitas ALCALDE, Lluisa PEREZ-GARCIA, Immaculada DINARES, Jordi FRIGOL ...1995 Volume 43 Issue 3 Pages 493-498
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of an ensemble of pyridinium(imidazolium) 4-nitrobenzimidazolate bentaines and their derivatives with several interannular linkages has been explored. Their antiprotozoal activity has also been examined.View full abstractDownload PDF (888K) -
Fumiko ABE, Rong-Fu CHEN, Tatsuo YAMAUCHI, Hiromu OHASHI1995 Volume 43 Issue 3 Pages 499-500
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS10-O-β-D-Glucopyranosyltheviridoside and 3'-O-β-D-glucopyranosyltheviridoside were obtained from the roots of Thevetia peruviana along with the major iridoids, theviridoside and theveside, and minor ones, recently obtained from the leaves, 10-O-fructofuranosyltheviridoside and 6'-O-glucopyranosyltheviridoside.View full abstractDownload PDF (378K) -
Takeo KAWAGUCHI, Hiroshi SAKAIRI, Shigeru KIMURA, Toyofumi YAMAGUCHI, ...1995 Volume 43 Issue 3 Pages 501-504
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3'-Amino-2', 3'-dideoxycytidine (8) was directly synthesized from 2'-deoxycytidine. 2', 3'-Dideoxy-3'-(N-acyl-L-phenylalanylamino)cytidines (acyl=butoxycarbonyl (9a), acetyl (9b), benzoyl (9c), and n-hexanoyl (9d)) were synthesized as chymotrypsin-activated prodrugs of 8. This N-protection was required for activation by chymotrypsin to 8. In vitro, compound 8 showed high cytotoxic activity against P388 cells, but the prodrugs 9a-d were ineffective. In vivo, however, these prodrugs showed much higher activity than 8 in mice bearing P388 cells.View full abstractDownload PDF (728K) -
Rate Constnats for Reaction of Hydroxyl Radicals with Water-Soluble Porphyrins and MetalloporphyrinsNoriko MOTOHASHI, Yutaka SAITO1995 Volume 43 Issue 3 Pages 505-507
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo determine the rate constants for the reaction of hydroxyl radicals with water-soluble porphyrins and their metalloporphyrins, tetrakis(4-sulfophenyl)porphine(TPPS), tetrakis(5-sulfothienyl)porphine (T(5-ST)P), tetrakis(4-N-methylpyridyl)porphine (TMPyP) and tetrakis(4-N-trimethylamino-phenyl)porphine (TTMAP), and Mn(III), Fe(III), Co(III) and Cu(II) complexes of TPPS and TMPyP, the γ-irradiation method, in which the fluorescence of hydroxybenzoates produced through reaction of benzoate with hydroxyl radicals generated by water-radiolysis is measured, were tried. However, since the porphyrins and metalloporphyrins show the characteristic absorption spectra in the visible region, the fluorescence of hydroxybenzoate products was disturbed by the colors. To separate the hydroxybenzoates from the colored solute, the products were extracted into ether under an acidic condition. The hydroxybenzoates were extracted thoroughly into the ether layer from an aqueous layer of less than pH 3 ; the residue was redissolved in phosphate buffer, pH 7.5; the solution was used to determine the rate constants. The rate constants for anionic porphyrins, TPPS, T(5-ST)P, were in the order of 109, and the constants for cationic porphyrins, TMPyP, TTMAP, in the order of 1010. Metal complexes of TPPS and TMPyP showed the rate constants of 6.9 to 11.4×109M-1S-1 and of 3.2 to 19.7×109M-1S-1, respectively.View full abstractDownload PDF (601K) -
Kiyotada YASUI, Hiroshi FUJIOKA, Yasuhiko NAKAMURA1995 Volume 43 Issue 3 Pages 508-511
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRecombinant human tumor necrosis factor-α (rHuTNF) was entrapped in liposomes consisting of Egg phosphatidylcholine (EggPC) alone, EggPC-egg phosphatidic acid (EggPA) or EggPC-egg phosphatidylglycerol (EggPG). These liposomes, stored in vials, were stable for a month at 4°C. The rHuTNF release from the liposomes were examined in rat plasma and phosphate buffered saline (PBS). rHuTNF was released from the liposomes containing EggPA in rat plasma. The release of rHuTNF was inhibited by EDTA and was induced in PBS containing CaCl2, indicating that this release is induced by Ca2+ ion in the plasma. The release of rHuTNF was promoted by an increase of the EggPA content.In conclusion, we could obtain stable liposomes in a vial and this liposome could immediately release rHuTNF in the rat plasma. Furthermore we were able to control the release rate of rHuTNF from these liposomes.View full abstractDownload PDF (578K) -
Albert J. LEO1995 Volume 43 Issue 3 Pages 512-513
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn a recent note to this journal Moriguchi et al. compared the reliability of several methods for calculating log P octanol/water from structure. The structures chosen were 22 drugs which Rekker and Manhold had analyzed earlier. On the basis of these values a statistical analysis indicated that the reliability of the methods decreased in the order : Moriguchi, Hansch, Rekker and Suzuki. The fact that regression equations relating measured to calculated values produced such unreasonably high deviations (s=0.764 to 1.240) and poor correlation coefficients (0.701 to 0.901) should have alerted the authors that some of the measured log P value were in error. Three major errors are apparent, and these affect the statistics to such an extent that the comparisons are not valid.View full abstractDownload PDF (362K) -
Tadashi MAKINO, Nobuyuki KITAMORI1995 Volume 43 Issue 3 Pages 514-516
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSLactose and ascorbic acid powders were granulated using corn or potato starch pastes. Starch pastes were cooked at different temperatures to obtain pastes of different degreees of gelatinization. The granules obtained were compressed into tablets and the hardness and disintegration time were examined. The gelatinization degree of starch paste was found to be closely related to the tablet properties, especially its disintegration time. An increase in gelatinization degree of the paste prolonged the disintegration time of the resultant tablets, although tablet hardness did not change. The relation between the gelatinzation degree of starch paste and tablet properties is discussed.View full abstractDownload PDF (664K) -
Osamu MURAOKA, Masafumi OKUMURA, Tomomi MAEDA, Lichen WANG, Genzoh TAN ...1995 Volume 43 Issue 3 Pages 517-519
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe photo-reaction of 9-oxabicyclo[3.3.1]nonan-3-one (2) was investigated. Upon irradiation in methanol, the ketone (2) predominantly gave the methanol adduct, 3-hydroxymethyl-9-oxabicyclo[3.3.1]nonan-3-ol (3), accompanied with photo-reduced products, exo- and endo-9-oxabicyclo[3.3.1]nonan-3-ol (4 and 5). Irradiation in water resulted in Norrish type I cleavage to give directly (cis-6-methyletrahydropyran-2-yl)acetic acid (1), a constituent of civet, in moderate yield.View full abstractDownload PDF (582K) -
Jun-ichi ANZAI, Hiroki TAKESHITA, Tomonori HOSHI, Tetsuo OSA1995 Volume 43 Issue 3 Pages 520-522
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn alternate and repeated deposition of avidin and biotinylated lactate oxidase (LOx) gave a thin film on the surface of platinum electrode. Amperometric response of L-lactate sensors thus prepared was enhanced stepwise by increasing the number of LOx layers. The enhanced response contributed to the extension of the lower detection limit of the sensor. The response time of the sensors was satisfactorily fast (ca. 10 s), irrespective of the number of LOx layers.View full abstractDownload PDF (464K) -
Tsuyoshi MIURA, Yukio MASAKI1995 Volume 43 Issue 3 Pages 523-525
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe catalytic activity of various types of capto-dative ethylenes has been investigated on alcoholysis of epoxides, and dicyanoketene dimethyl acetal (DCKDMA) and dicyanoketene ethylene acetal (DCKEA) are found to be efficient and mild catalysts.View full abstractDownload PDF (441K) -
Hirohito IKEDA, Toru HARAGUCHI, Miho YUKAWA, Tokihiro NIIYA, Yoshinobu ...1995 Volume 43 Issue 3 Pages 526-528
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNitrosation of α, α'-dianions produced from ketones using a couple of bases was carried out with tert-butyl nitrite(tert-BuONO) in ether, and then two regioisomers of oximes(but not acetone)were obtained simultaneously. The ratio of these regioisomers was remarkably reversed by the addition of hexamethylphosphoric triamide(HMPA).View full abstractDownload PDF (420K) -
Takashi WATANABE, Jin HASEGAWA, Kou HIROYA, Kunio OGASAWARA1995 Volume 43 Issue 3 Pages 529-531
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDiastereomerically pure tranexamic acid has been prepared via a diastereomeric separation of a trans-/cis-mixture of 1, 4-cyclohexanedimethanol using lipase PS (Pseudomonas sp. Amino).View full abstractDownload PDF (419K) -
Masayuki YOSHIKAWA, Tomohiko UEDA, Osamu MURAOKA, Hiroshi AOYAMA, Hisa ...1995 Volume 43 Issue 3 Pages 532-534
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo bioactive novel triterpene glycosides named hovenidulciosides A1 and A2 have been isolated from a Chinese natural medicine, Hoveniae Semen Seu Fructus, the seeds and fruit of Hovenia dulcis Thunb. (Rhamnaceae). The absolute stereostructures of hovenidulciosides A1 and A2 with a migrated 16, 17-seco-dammarane skeleton have been determined on the basis of chemical and physicochemical evidence which included the X-ray crystallographic analysis of the p-bromobenzoate of their common aglycone, hovenidulcigenin A. Hovenidulciosides A1 and A2 exhibited inhibitory activity on the histamine release from rat mast cells induced by compound 48/80 or calcium ionophore A-23187.View full abstractDownload PDF (494K) -
Yasushi ARAKAWA, Takahiro GOTO, Kazuya KAWASE, Shigeyuki YOSHIFUJI1995 Volume 43 Issue 3 Pages 535-536
Published: March 15, 1995
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hetero Diels-Alder adducts 1 derived from azodibenzoyl and cyclic dienes were transformed to the meso-diaminodicarboxylic acids 6 via the new cyclic hydrazoacetic acids 3.View full abstractDownload PDF (371K)
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