巻号一覧
46 巻, 3 号
選択された号の論文の36件中1～36を表示しています
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Shigenori OKA, Kunihiko TAJIMA, Hiromu SAKURAI1998 年 46 巻 3 号 p. 377-383
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーTo understand the activation of molecular dioxygen by the heme-containing enzyme tryptophan 2, 3-dioxygenase (TDO), a chemical model was constructed, which permitted an identification of reactive intermediates through the use of ESR, optical spectra, cyclic voltammetry, and oxygenated product analysis. The temperature-dependent ESR measurement for the chemical model, which consisted of tetraphenylporphine iron(III) chloride (Fe(III)TPPCl), 3-methylindole (skatole; Sk), tetramethylammonium hydroxide (TMAOH), and molecular dioxygen, revealed the generation of two kinds of free radical species, as well as the formation of two ternary complexes in the ferric low-spin state. The radical species R1, with an ESR value of g=2.0045, was determined to be a Sk neutral radical derived from the substrate by MO calculation. The radical species R2, with an ESR value of g=2.015 was indicated to be a Sk-peroxide radical, consisting of a dioxygen molecule bound to the Sk neutral radical. A comparison of the ESR parameters of the two ternary complexes with those of previously reported complexes suggested that the present complexes are six-coordinate ferric low-spin species : one which is bound with two dioxygenated Sk anions at the heme-iron site ([A] : g1=2.236, g2=2.160, g3=1.965), and the other bound with a dioxygenated Sk anion and a methoxide anion ([B] : g1=2.311, g2=2.160, g3=1.954). These ternary complexes are assumed to be possible models for the transient hemoprotein-peroxide complexes. The formations of R1 and ternary complexes were indispensable for the dioxygenation of the substrate. On the basis of these results, a possible reaction mechanism is proposed.抄録全体を表示PDF形式でダウンロード (1043K) -
Takayasu YAMAUCHI, Hiroshi TAKAHASHI, Kimio HIGASHIYAMA1998 年 46 巻 3 号 p. 384-389
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーChiral 1, 3-oxazolidines having a diphenylmethyl group at the 3-position of the oxazolidine ring as a bulky substituent were synthesized. The reaction of Grignard reagents with the chiral 1, 3-oxazolidines afforded the corresponding amines with very high diastereoselectivity. Furthermore, the method for the synthesis of optically active amines was applied to the asymmetric synthesis of (-)-dihydropinidine, a piperidine alkaloid.抄録全体を表示PDF形式でダウンロード (1006K) -
Akira MIYASHITA, Yumiko SUZUKI, Ken-ichi IWAMOTO, Takeo HIGASHINO1998 年 46 巻 3 号 p. 390-399
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーIn the presence of 1, 3-dimethylimidazolium iodide (1), 6-chloro-9-phenyl-9H-purine (7) and 4-chloro-5, 6-dimethylpyrrolo[2, 3-d]pyrimidines 40-42 undrwent uncleophilic aroylation with arenecarbaldehydes (5) to give the corresponding fused aroylpyrimidines 8 and 43-45. 1, 3-Dimethylbenzimidazolium iodide (2) was an effective catalyst for the similar synthesis of 7-aroyl-3-phenyl-3H-1, 2, 3-triazolo[4, 5-d]pyrimidines 16-21. In the synthesis of 4-aroyl-1H-pyrazolo[3, 4-d]pyrimidines 26-32, both azolium salts 1 and 2 were effective as catalysts. Moreover, 4-aroyl-7H-pyrrolo[2, 3-d]pyrimidines 43-45 were obtained in good yields via the 4-tosyl derivatives, in the presence of catalytic amounts of sodium p-toluenesulfinate (46) and the imidazolium salt 1. This catalytic aroylation was found to be a facile and useful method for the synthesis of 6-aroyl-9H-purines and their analogues.抄録全体を表示PDF形式でダウンロード (1298K) -
Hideaki MURATAKE, Miyuki TONEGAWA, Mitsutaka NATSUME1998 年 46 巻 3 号 p. 400-412
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーFormal syntheses of (±)-duocarmycin SA, natural (+)-duocarmycin SA and unnatural (-)-duocarmycin SA were accomplished by way of a tricyclic heteroaromatic compound 10b. For the preparation of 10, an N-oxide route aiming at a process 20 in Chart 3 was first investigated by synthesizing 19, derived from Stille coupling products 13 between bromopyrrole 7a and 3-(tributylstannyl)pyridines 12, but without success. As the second approach, Stille coupling products 9a-c were prepared by condensation between 7a and 2-substituted 3-(trialkylstannyl)pyridines 8a-f. Both 9b and 35, derived from 9c, were converted to their silyl enol ethers and then subjected to a palladium-catalyzed methyl ketone-arylation reaction in the presence of tributyltin fluoride and lithium chloride, affording 10a and 10b in excellent yields, especially from 35. Application to 10b of three successive operations, i.e., i) partial reduction of 10b to dihydropyridine derivatives 11a and 11b, ii) dihydroxylation of the double bonds formed to give 58 and 59, and iii) reductive elimination of the hydroxy groups adjacent to the nitrogen function and the aromatic ring, afforded 6 in fairly good yield. Compound 6 was readily converted to relay compounds 64 and 67, completing total syntheses of (±)-, (+)-, and (-)-duocarmycin SA. Both Sharpless asymmetric dihydroxylation (AD) and Jacobsen's asymmetric epoxidation were applied to 11a and 11b. At the best, 81% ee was observed in the AD reaction of 11a using 2, 5-diphenyl-4, 6-bis(9-O-dihydroquinyl)pyrimidine [(DHQ)2PYR], but the resulting 58 possessed an unnatural absolute configuration.抄録全体を表示PDF形式でダウンロード (2243K) -
Tian-Shung WU, Hua-Chun HSU, Pei-Lin WU, Yann-Lii LEU, Yu-Yi CHAN, Chi ...1998 年 46 巻 3 号 p. 413-418
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーReinvestigation of the root of Rhinacanthus nasutus afforded, in addition to rhinacanthin-A to -D reported previously, two new dimethyldihydropyranonaphthoquinone esters (5, 6) and eight new 2-hydroxy-1, 4-naphthoquinone esters (7-14) were isolated. The stereochemistry of rhinacanthin-A was determined as the R configuration. Compounds rhinacanthin-G to N, belong to a class of 2-hydroxy-3-(3-hydroxy-2, 2-dimethylpropyl)-1, 4-naphthoquinone esters, and so far have been isolated only in this plant. Their biosynthesis is also discussed.抄録全体を表示PDF形式でダウンロード (864K) -
Masumi TAKEMOTO, Yuichi YAMAMOTO, Kazuo ACHIWA1998 年 46 巻 3 号 p. 419-422
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーWe have synthesized optically active α-(p-chlorophenyl)pyridylmethanols by reduction or by hydrolysis with plant cell cultures.抄録全体を表示PDF形式でダウンロード (664K) -
Haruhiro FUJIMOTO, Junko NAGANO, Kentaro YAMAGUCHI, Mikio YAMAZAKI1998 年 46 巻 3 号 p. 423-429
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーTwo known fungal metabolites, macrophin and colletodiol, and a new stereoisomer of colletodiol named 10-epi-colletodiol, were isolated as immunosuppressive principles from an Ascomycete, Diplogelasinospora grovesii. The IC50 values of the major active component among them, macrophin, were calculated to be 0.4 and 0.3μg/ml against concanavalin A- and lipopolysaccharide-induced proliferations of mouse spleen lymphocytes, respectively. A new natural product, 4, 8-dimethyl-1, 5-dioxacyclooctane-2, 6-dione, and a known fungal metabolite, isosclerone, which showed no immunosuppressive activity, were also isolated from this fungus.抄録全体を表示PDF形式でダウンロード (949K) -
Tatsumi SHINOHARA, Akira TAKEDA, Jun TODA, Takehiro SANO1998 年 46 巻 3 号 p. 430-433
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe conformation of the piperideine ring in 1-benzyl-1, 2, 3, 4-tetrahydroisoquinolines was determined as 2H3 form with a pseudoaxial position of the 1-benzyl group by circular dichroism (CD) spectral comparison with 1-methyl-1, 2, 3, 4-tetrahydroisoquinolines. The chiral center at C-1 of 1, 2, 3, 4-tetrahydroisoquinoline (TIQ) was constructed in an unambiguous manner by applying a new method of TIQ synthesis utilizing the Pummerer reaction as a key step. Enantiomerically pure (R)- and (S)-1-methyl- and 1-benzyltetrahydroisoquinolines (1) were prepared starting from readily available chiral amines (2) in good overall yields.抄録全体を表示PDF形式でダウンロード (722K) -
Yasuyuki TAKEDA, Keiichi KAWAGOE, Aki YOKOMIZO, Yoshihiro YOKOMIZO, To ...1998 年 46 巻 3 号 p. 434-444
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーA novel series of phenoxyacetic acid derivatives was synthesized based on considerations of the three-dimensional structural similarity of YM022 and RP72540. The gastrin/cholecystokinin (CCK)-B and CCK-A receptor antagonist activities of these compounds were evaluated by investigation of their affinities for human gastrin/CCK-B receptors and human CCK-A receptors, respectively. It was found that N-methyl-N-phenyl-2-[2-[N-(N-methyl-N-phenyl-carbamoylmethyl)-N-[2-[3-(3-methylphenyl)ureido]acetyl]amino]phenoxy]acetamide (20k, DZ-3514) exhibited high affinity for gastrin/CCK-B receptors and high selectivity over CCK-A receptors.抄録全体を表示PDF形式でダウンロード (1500K) -
Megumi YAMADA, Yasuo SATO, Kazuko KOBAYASHI, Fukio KONNO, Tomoko SONED ...1998 年 46 巻 3 号 p. 445-451
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーSeveral modified 2-piperazinyl benzoxazole derivatives, which exhibit an agonistic effect on gastrointestinal motility, were synthesized and their effects on the contraction of guinea-pig ileum were examined. The quaternary piperazinyl benzoxazole structure has a restricted conformation and stereostructure compared to those of the other 5-HT3 receptor agonists, serotonin and meta-chlorophenylbiguanide. The mutual positions of the aromatic ring, nitrogen atom and terminal amine are considered to form the pharmacophore of the 5-HT3 receptor agonist in the gut. In the serotonin-evoked reflex bradycardia [Bezold-Jarisch (B-J) reflex] inhibition test using rats the B-J reflex-inducing ratio was different for each synthesized compound. These results suggest that, in these 5-HT3 receptor agonists, the substituents of the benzoxazole ring influence the B-J reflex-inducing activity in rats.抄録全体を表示PDF形式でダウンロード (1038K) -
Yuko TSUDA, Keiko WANAKA, Mayako TADA, Shosuke OKAMOTO, Akiko HIJIKATA ...1998 年 46 巻 3 号 p. 452-457
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe synthetic plasma kallikrein (PK) inhibitor trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxymethylanilide (PKSI-527) consists of three parts. Each part was replaced by analogues in an attempt to improve the potency and the selectivity of PKSI-527. Among the peptides examined, trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxyanilide (peptide 16) inhibited PK with a high selectivity and an IC50 value of 2.7μM, being as potent as PKSI-527.抄録全体を表示PDF形式でダウンロード (905K) -
Hidehito URATA, Hidetaka MIYAGOSHI, Hitoshi KAKUYA, Hideki TOKUMOTO, T ...1998 年 46 巻 3 号 p. 458-461
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーCarbocyclic pyrimidine nucleoside analogs which have restricted glycosidic conformation at X≈180° were designed, based on the conformational features of the L-nucleotide residue in heterochiral DNA, and synthesized. The synthesis of (±)-carbocyclic 6, 6'-O-cyclo-2'-deoxyuridine was achieved via bromination and subsequent intramolecular cyclization of carbocyclic 6'β-hydroxy-2'-deoxyuridine. (±)-Carbocyclic 6, 6'-O-cyclo-2'-deoxycytidine was synthesized from protected carbocyclic 6, 6'-O-cyclo-2'-deoxyuridine via the 4-triazole intermediate.抄録全体を表示PDF形式でダウンロード (708K) -
Mami TAKIKAWA, Kiyoko UNO, Takashi OOI, Takenori KUSUMI, Shusaku AKERA ...1998 年 46 巻 3 号 p. 462-466
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーPolydora websterii, a harmful lugworm that has serious adverse effects on pearl oyster cultivation, was inhibited by a marine diterpene, crenulacetal C, isolated from the brown alga Dictyota dichotoma, Based on consideration of the activity-structure relationship, several synthetic compounds having an aromatic moiety with a hydroxyalkyl chain were prepared. Bioassay using larvae of Polydora websterii as well as pearl oysters (Pinctada fucata martensii) suggested that 1-(2-furyl)-1-nonanol was the most promising inhibitor.抄録全体を表示PDF形式でダウンロード (788K) -
Akiko KUSANO, Masayuki TAKAHIRA, Makio SHIBANO, Yasuko IN, Toshimasa I ...1998 年 46 巻 3 号 p. 467-472
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe absolute stereostructues of cimicifugoside (1) and actein (2) from Cimicifuga simplex were established by X-ray crystal analysis of 26(S)-O-methylcimicifugenin A (1cS) prepared from 1, negative CD curves of 26-O-methyl-3-keto-cimicifugenins (1dS, 1dR), comparative analysis of 1H- and 13C-NMR spectra of 1, 2 and their derivatives, and preparation of 2 from 1 by hydrogenation : 20(R), 23(R), 24(R), 25(S), 26(R, S)-16β : 23; 23 : 26; 24 : 25-triepoxy-12β-acetoxy-3β, 26-dihydroxy-9, 19-cyclolanost-7-ene 3-O-β-D-xylopyranoside for 1 and 20(R), 23(R), 24(R), 25(S), 26(R, S)-16β : 23; 23 : 26; 24 : 25-triepoxy-12β-acetoxy-3β, 26-dihydroxy-9, 19-cyclolanostane 3-O-β-D-xylopyranoside for 2.抄録全体を表示PDF形式でダウンロード (869K) -
Yasuo YOSHIHASHI, Midori MAKITA, Shigeo YAMAMURA, Eihei FUKUOKA, Katsu ...1998 年 46 巻 3 号 p. 473-477
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーA method of measuring the rate of water penetration into tablets was proposed in which a heat conduction microcalorimeter was employed. Heat evolved when the tablets were immersed in water. The rate of generation of the heat was determined by a deconvolution method. The rate of water penetration into tablets when they were placed in water was determined by assuming to correspond to the generation rate of heat. For model experiments of water penetration into tablets, hydrophilic MCC was used as a basic component of the tablet, and hydrophobic phenytoin as an active ingredient. The time required for total water penetration of MCC tablets increased with tablet compression pressure, and the rate of water penetration into the tablets increased with phenytoin content.抄録全体を表示PDF形式でダウンロード (683K) -
Chun-Ren CHEN, Shu-Ling CHO, Chih-Kuang LIN, Yaw-Hung LIN, Shu-Tuan CH ...1998 年 46 巻 3 号 p. 478-481
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe disintegration and dissolution of acetaminophen tablets containing sucrose and Ac-Di-Sol/Primojel was significantly different between acidic and neutral media. The purpose of this study was to investigate the mechanism of this phenomenon and to propose a way of reducing the dissolution difference between the two media. Tablets of different combinations of active ingredient, sucrose, and Ac-Di-Sol/Primojel were prepared and their dissolution in various media was evaluated. The dissolution differences were found to be largely related to the hydrophobicity of the active ingredient and pH difference of the two media. This difference was even more evident under the condition where acetaminophen, sucrose, and Primojel were combined. The dissolution difference was therefore attributed to the depressed function of Primojel in the acidic medium, the stronger binding of sucrose, the hydrophobicity of the active ingredient and pH difference of the two media. Increasing the concentration of Primojel or incorporating the surfactant in the tablet can thus greatly decrease the dissolution difference between acidic and neutral media.抄録全体を表示PDF形式でダウンロード (623K) -
Hideshi SUZUKI, Hisakazu SUNADA1998 年 46 巻 3 号 p. 482-487
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe objective of this investigation was to clarify the influence of water-soluble polymers on the dissolution behavior of nifedipine from solid dispersions with combined carriers. All the solid dispersions of nifedipine were prepared by the fusion method using nicotinamide and 4 different water-soluble polymers, hydroxypropylmethylcellulose (HPMC), polyvinylpyrrolidone (PVP), partially hydrolyzed polyvinyl alcohol (PVA) and pullulan. HPMC, PVP or PVA dissolved in the fused liquid of nicotinamide and operated efficiently on the amorphous formation of nifedipine in solid dispersions. In dissolution studies, the drug concentration for these dispersions increased to more than twice intrinsic drug solubility. The rank order of the drug concentration was HPMC>PVP>PVA. However, since pullulan did not dissolve in the fused nicotinamide, nifedipine was present as a crystalline state in the solid dispersion; the supersaturation behavior of the drug was scarcely observed. The compatibility, namely, the solubility and miscibility, between nicotinamide or nifedipine and the polymers, was determined by differential scanning calorimetry using the mixtures treated with fusing and subsequent rapid cooling. Both HPMC and PVP exhibited high compatibility not only with nicotinamide but also with nifedipine. The crystallization behavior of nifedipine from a supersaturated solution containing nicotinamide or the polymers was studied. The inhibitory effect of HPMC or PVP for drug crystallization was evident, which would be related not to the solubilizing effect but to the adhesive force of the polymer for the drug. Therefore, it was understood that the use of a polymer with high compatibility and adhesion with nifedipine provides a high supersaturation level of the drug in dissolution. Further, the solubility parameter was found to be useful for selecting a suitable polymer as a component of combined carriers.抄録全体を表示PDF形式でダウンロード (954K) -
Hiroyasu KOKUBO, Chinatsu NAKASHIMA, Hisakazu SUNADA1998 年 46 巻 3 号 p. 488-493
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーA model system consisting of lactose-cornstarch was used to examine the effect of five cellulosic binders [hydroxypropylcellulose (HPC)(6cP), hydroxypropylmethylcellulose 2910 (HPMC)(3, 6, 15cP) and methylcellulose (MC)(15cP)] on the particle size distribution of granules prepared in an agitating fluidized bed under fixed operating conditions. The distribution of binder in different size fractions of granules was also determined by measuring the contents of methoxyl and hydroxypropoxyl groups. When the binders were added by the solution method, higher solution viscosity resulted in the granule size being increased, with almost equivalent binder distributions in different size fractions. The granules prepared by the dry mixing method with HPC (6cP) or HPMC (3cP) also showed a good correlation between median particle size and binder level, though the binders were concentrated in the coarse-sized particle fractions of the granules. The results are consistent with our previous findings on wet granulation with a fluidized bed. When a trace amount of water-soluble dye was mixed with the granulating liquid or powder components to examine the granulation mechanism in both the solution and the dry mixing methods of binder addition, the dye distributions were more uniform than the binder distributions, especially in the dry mixing method. This suggests that the solubility of binders or dye in water is a critical factor determining their distribution in the different size fractions of the granules.抄録全体を表示PDF形式でダウンロード (786K) -
Makiko YAMADA, Yoshiaki KATO, Mikio NAKAMURA, Takashi YAMADA, Tamio MA ...1998 年 46 巻 3 号 p. 494-499
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーMajor subsidiary colors A (Sub A) and B (Sub B) in commercial Food Red No.102, and colors C (Sub C) and D (Sub D) in commercial Foor Red No.2 were isolated. These structures were characterized by physicochemical evidence. The structures of Sub A, B, and C are trisodium salt of 7-hydroxy-8-(6-sulfonaphthyl-2-azo)-1, 3-naphthalenedisulfonic acid, disodium salt of 4-amino-3-(4-sulfonaphthyl-1-azo)-1-naphthalenesulfonic acid and trisodium salt of 3-hydroxy-4-(6-sulfonaphthyl-2-azo)-2, 7-naphthalenedisulfonic acid, respectively. Sub D was identified as Sub B.抄録全体を表示PDF形式でダウンロード (782K) -
Rena KASIMU, Ken TANAKA, Yasuhiro TEZUKA, Zhu-Nan GONG, Jian-Xin LI, P ...1998 年 46 巻 3 号 p. 500-504
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe dry root and rhizome of Salvia miltiorhiza (Lamiaceae) are used as a crude drug Danshen, while those of S. deserta (Xinjiang-Danshen) are mixed in Danshen at Xinjiang province when the former is in short supply. The water and MeOH extracts of S. deserta showed strong aldose reductase (AR) inhibitory activity, and their active constituents were determined to be polar compounds different from "tanshinones" of S. miltiorhiza, i.e., lithospermic acid B (1), salvianolic acid K (2), salviaflaside (3), and rosmarinic acid (4) (IC50, 2.63-3.91μM).We also examined the AR inhibitory activity of water and MeOH extracts of seventeen Salvia plants, including ten species of Danshen resources (S. bowleyana, S. deserta, S. miltiorhiza, S. miltiorhiza var. miltiorhiza f. alba, S. paramiltiorhiza, S. paramiltiorhiza f. purpureo-rubra, S. przewalskii, S. przewalskii var. mandarinorum, S. sinica f. purpurea, S. trijuga), and their water extracts were also analyzed by liquid chromatography-mass spectrometry (LC-MS). The results indicated that there were four types with regard to the AR inhibitory activity and three types with regard to the amount of 1. Ten species used as Danshen resources showed good correlation between the AR inhibitory activity and the morphological classification. However, the intensities of their AR inhibitory activity varied, and they contained 1 in varying amounts. These facts suggested that the ten species were not the same, and thus their use as a Danshen resource should be based on their activity and/or active constituents.抄録全体を表示PDF形式でダウンロード (739K) -
Kazuhiro KITAORI, Yoshikazu TAKEHIRA, Yoshiro FURUKAWA, Hiroshi YOSHIM ...1998 年 46 巻 3 号 p. 505-507
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリー(R)- or (S)-Atenolol (1) in enantiopure form was prepared in an extremely simple way. Atenolol of ca. 95% ee was prepared in one-pot from p-hydroxyphenylacetamide (2) and (R)- or (S)-epichlorohydrin (3). Then, preferential crystallization of the Bronsted's acid salts of the resulting atenolol improved the enantiomeric purity up to 99.8% ee.抄録全体を表示PDF形式でダウンロード (496K) -
Yasuhiro MAEDA, Yoshiro SATO1998 年 46 巻 3 号 p. 508-511
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーReaction of N, N-dimethyl-N-(tributylstannyl)methyl-4-substituted benzylammonium salts 2 with lithium diisopropylamide (LDA) gave N, N-dimethyl-2-(tributylstannyl)methyl-5-substituted benzylamines 3 as the main products. Treatment of 3 with iodomethane followed by tetrabutylammonium fluoride (TBAF) in the presence of dimethyl fumarate gave the corresponding dimethyl trans-1, 2, 3, 4-tetrahydro-6-substituted naphthalene-2, 3-dicarboxylates 15 in good yields.抄録全体を表示PDF形式でダウンロード (740K) -
Zhi-Hong JIANG, Chizuko INUTSUKA, Takashi TANAKA, Isao KOUNO1998 年 46 巻 3 号 p. 512-513
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThree new triterpenes and a new triterpene ferulate were isolated from the bark of Rhoiptelea chiliantha DIELS et HAND.-MAZZ.(Rhoipteleaceae). Their structures were elucidated on the basis of spectral and chemical evidence.抄録全体を表示PDF形式でダウンロード (436K) -
Tokujiro KITAGAWA, Chinatsu TSUTSUI, Kumi HAYASHI, Aiko YAMANO1998 年 46 巻 3 号 p. 514-517
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーN'-Substituted N-furfuryloxamides (4) were prepared via condensation of potassium methyl oxalate (8) with furfurylamine (5f) using 1, 1'-oxalyldiimidazole (6), followed by hydrolysis of the resulting amide-ester (10), and finally condensation with aliphatic or aromatic amines (5). The prepared compounds (4) were examined for activity as plant growth regulators using two kinds of plant seeds, namely, those of rape, Brassica campestris L. (Dicotyledoneae) and leek, Allium tuberosum ROTTLER (Monocotyledoneae). N'-Benzyl- and N'-phenyl-N-furfuryloxamides (4b and 4c) and N, N'-difurfuryloxamide (4f) inhibited root growth in seedlings of both species.抄録全体を表示PDF形式でダウンロード (649K) -
Kiyoshi IKEDA, Tatsuhisa KATO, Takehisa SUZUKI, Kazuo ACHIWA1998 年 46 巻 3 号 p. 518-522
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーLipase-catalyzed enzymatic hydrolysis of dimethyl esters of 1, 4-dihydropyridines to the monoester, which is an important intermediate for the synthesis of optically active 1, 4-dihydropyridines, does not proceed directly. This paper describes the design and synthesis of novel haptens having a phosphonate group containing the requisite oxyanionic character to mimic the tetrahedral intermediate of hydrolysis, and the application of these compounds for generating antibodies with catalytic ability for the enantioselective partial hydrolysis of the dicarboxylic dimethyl ester (1) of a 1, 4-dihydropyridine derivative to generate the monocarboxylic acid (2).抄録全体を表示PDF形式でダウンロード (744K) -
Keisuke KOJIMA, Kimio ISAKA, Yukio OGIHARA1998 年 46 巻 3 号 p. 523-525
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーFive new tetranortriterpenoids, methyl 3β-tigloyloxy-2, 6-dihydroxy-1-oxo-meliac-8(30)-enate, methyl 3β-tigloyloxy-2-hydroxy-1-oxo-meliac-8(30)-enate, methyl 3β-tigloyloxy-2-hydroxy-8α, 30α-epoxy-1-oxo-meliacate, methyl 3β-acetoxy-2, 6-dihydroxy-8α, 30α-epoxy-1-oxo-meliacate and methyl 3β-isobutyryloxy-2, 6-dihydroxy-8α, 30α-epoxy-1-oxo-meliacate, were isolated from the seeds of Swietenia macrophylla. The structure of these five tetranortriterpenoids was established by comprehensive spectral analysis.抄録全体を表示PDF形式でダウンロード (508K) -
Manabu UDAYAMA, Junei KINJO, Naotoshi YOSHIDA, Toshihiro NOHARA1998 年 46 巻 3 号 p. 526-527
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーA new oleanene glucuronide called melilotus-saponin O1 (1) was isolated together with three known ones from the roots of Melilotus officinalis (L.) PALLAS (Leguminosae). The structure of 1 was determined to be 3-O-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→3)]-β-D-galactopyranosyl-(1→2)-β-D-glucuronopyranosyl soyasapogenol B by spectroscopic and chemical methods.抄録全体を表示PDF形式でダウンロード (441K) -
Fumiyuki KIUCHI, Yumi FUKAO, Takuro MARUYAMA, Tohru OBATA, Motohiro TA ...1998 年 46 巻 3 号 p. 528-530
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThree cardenolide glycosides, calotropin (1), frugoside (2), and 4'-O-β-D-glucopyranosylfrugoside (3), were obtained as the cytotoxic principles of "akond mul" (roots of Calotropis gigantea L.). The cytotoxicity of these compounds against various cell lines of human and mouse origin was tested. They showed similar cell line selectivity to those of cardiac glycosides such as digoxin and ouabain : they are toxic to cell lines of human origin, but not to those from mouse at 2μg/ml.抄録全体を表示PDF形式でダウンロード (599K) -
Toru MAEJIMA, Takashi OSAWA, Kingo NAKAJIMA, Masao KOBAYASHI1998 年 46 巻 3 号 p. 531-533
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーA new coating method for use in preparing controlled-release beads was developed by modifying the tumbling melt granulation technique. The dissolution rate of the drug from the beads was controlled by coating the mixture of meltable and non-meltable materials by heating in a centrifugal fluidizing granulator without using any solvent. In experiments using talc as the non-meltable material, the resultant beads showed the sufficient ability to suppress the dissolution of the drug and no change in the dissolution characteristics by wetting agent and in a stability test at high temperature. Using functional polymer as the non-meltable material, the controlled-release beads with various dissolution characteristics could be prepared : entero-soluble-release beads using entero-suluble polymer, and zero-order-release beads using hydrophilic gel-forming agent and talc.抄録全体を表示PDF形式でダウンロード (775K) -
Toru MAEJIMA, Masashi KUBO, Takashi OSAWA, Kingo NAKAJIMA, Masao KOBAY ...1998 年 46 巻 3 号 p. 534-536
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe tumbling melt granulation (TMG) method was applied to prepare controlled-release fine granules of diltiazem hydrochloride (DH). The entire process, from the preparation of the cores by the adherence of DH to the sucrose crystal to the subsequent coating of the controlled-release layer, was performed without using any solvent. A mixture of meltable material, talc, and ethylcellulose was used for the controlled-release layer and controlled-release fine granules approximately 400μm in diameter were obtained with excellent producibility. The dissolution rate of DH from these fine granules was similar to that of a once-a-day dosage form obtained in the merket; further, the dependency of the dissolution profile on pH of the media was less. Thus, it was concluded that this TMG method was very useful for preparing not only controlled-release beads of granule size (usually 500 to 1400μm) but also fine granules.抄録全体を表示PDF形式でダウンロード (734K) -
Tapan Kumar SAHA, Kaori JONO, Hideki ICHIKAWA, Yoshinobu FUKUMORI1998 年 46 巻 3 号 p. 537-539
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーChitosan microspheres (CMSs) containing water-soluble gadolinium diethylenetriaminepentaacetic acid (Gd-DTPA) were prepared by an emulsion method using Span 80 as a surfactant and glutaraldehyde (GA) as a cross-linker for the gadolinium neutron-capture therapy of cancer. When Gd-DTPA was applied at more than a 1 : 1 number ratio of its carboxylic groups to the amino groups of chitosan, the content of Gd in CMS was saturated at about 13% and the mass median diameter of CMS was increased beyond that of placebo CMS. The increase in the amount of Span 80 and GA applied led to a decrease in the CMS size and hte Gd content. The electrostatic interaction between chitosan and Gd-DTPA and the preferential surface-hardening by GA contributed to the formation of fine, spherical, Gd-enriched and prolonged-releasing CMSs with a mass median diameter of 1.9μm, a Gd content of 6.1% and a 50% dissolution time of 2.4h.抄録全体を表示PDF形式でダウンロード (720K) -
Izumi TANEMURA, Yoshihiro SAITO, Haruhisa UEDA, Takatoshi SATO1998 年 46 巻 3 号 p. 540-541
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe stability constants for the inclusion of fragrance materials with 2-hydroxypropyl-β-cyclodextrin (2HP-β-CyD) in aqueous solution have been determined at 25°C by a solubility method. The solubility of fragrance in 2HP-β-CyD solution was determined from the concentration of fragrance in vapor which was in equilibrium with that in the solution using static head-space gas chromatography (SHSGC). The stability constants of (+)-limonene and linalool obtained by this method were in rough accord with the reported values. Because of its advantages of simplicity, less amount of guest used and the ease of temperature control, it was concluded that the SHSGC method is another useful technique for determining the solubility and stability constant of a volatile guest/CyD system in aqueous medium.抄録全体を表示PDF形式でダウンロード (425K) -
Masao TOYOTA, Chiyo NISHIMOTO, Yoshinori ASAKAWA1998 年 46 巻 3 号 p. 542-544
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe diethyl ether extract of the Japanese liverwort Frullania tamarisci subsp. obscura yielded a new sesquiterpene aldehyde in addition to a new dimeric sesquiterpenoid with a eudesmane-type carbon skeleton. Their structures were established by extensive 2D NMR techniques and chemical evidence. They were shown to be 4α, 6α-dihydroxy-11(13)-eudesmen-12-al and its dimer with 4-epi-arbusculin A at the C-4 ether linkage.抄録全体を表示PDF形式でダウンロード (454K) -
Yoshiyasu FUKUYAMA, Hiroyuki MINAMI, Isuzu YAMAMOTO, Mitsuaki KODAMA, ...1998 年 46 巻 3 号 p. 545-547
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーNeovibsanins H (1) and I (2), novel vibsane-type diterpenes, have been isolated from the leaves of Viburnum awabuki and their structures have been elucidated by spectroscopic analyses. The absolute configuration of 1 has been determined by applying the modified Mosher's method.抄録全体を表示PDF形式でダウンロード (407K) -
Roland BARRET, Nathalie ROUE, H. FILLION1998 年 46 巻 3 号 p. 548-550
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーThe hetero Diels-Alder reaction of 4, 7-indoloquinones with crotonaldehyde dimethylhydrazone afforded 5-methyl-5, 6-dihydropyrido[6, 5-b]indole-4, 9-dione ([1, 8] isomer) and 5-methyl-5, 6-dihydropyrido[5, 6-b]indole-4, 9-diones ([1, 5] isomer). The 6, 7, 8, 9-tetrahydrocarbazole-2, 5-dione region-selectively afforded 4-methyl-1, 4, 6, 7, 8, 9-hexahydropyrido[2, 3-b]carbazole-5, 11-dione. The regiochemistry of these reactions was controlled by the substitution of the nitrogen and the 2-C atom of the indole moiety : the unsubstituted quinones afforded the [1, 8] regioisomer, whereas the [1, 5] compounds were obtained with the quinones bearing an electron-withdrawing substituent on the nitrogen or the 2-C atom.抄録全体を表示PDF形式でダウンロード (420K) -
REDUCTION OF Mn3+-TETRAKIS(4-METHYLPYRIDYL)PORPHINE WITH ALBUMIN OBSERVED IN RESONANCE RAMAN SPECTRANoriko MOTOHASHI, Toyohiro HINOKIYAMA, Masako HIGASHI, Masaki MIFUNE, ...1998 年 46 巻 3 号 p. 551-553
発行日: 1998/03/15
公開日: 2008/03/31
ジャーナル フリーWhen the resonance Raman spectra of Mn3+-tetrakis(4-methylpyridyl)-porphine are measured in the presence of albumins, the resonance Raman bands of Mn2+-tetrakis(4-methylpyridyl)porphine are frequently observed. This reduction of Mn3+to Mn2+ could be caused by an action of unfolding albumins resulting from heat and/or light.抄録全体を表示PDF形式でダウンロード (498K)
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