巻号一覧
31 巻, 10 号
選択された号の論文の64件中1～50を表示しています
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井上 正美, 太田 健治, 石塚 [なお]康, 榎本 三郎1983 年 31 巻 10 号 p. 3371-3376
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーChiral rhodium (I) complexes of (-)-2, 3-O-isopropylidene-2, 3-dihydroxy-1, 4-bis (diphenylphosphino) butane (DIOP) and (2S, 4S) -N-butoxycarbonyl-4-diphenylphosphino-2-diphenyl-phosphinomethylpyrrolidine (BPPM) were fixed on charcoal which had been pretreated with metal acetates and triethylamine, and the hydrogenation of α-acetamidocinnamic acid was performed in an ethanol-H2O (1 : 1) mixture. L-N-Acetyl- (R) -phenylalanine was obtained in optical yields of 70.5% with RhCl (COD) -DIOP-charcoal catalyst and 86.5% with RhCl (COD) -BPPM-charcoal catalyst. The optical yields were affected by hydrogen pressure, reaction temperature, the concentration of the substrate, and the composition of the solvent. The recovered catalyst retained its activity well and could be re-used repeatedly for enantioface-differentiating hydrogenation, provided that it was kept under a nitrogen atmosphere throughout.抄録全体を表示PDF形式でダウンロード (640K) -
塚本 豊久, 野村 英城, 森田 修之, 岡田 壽太郎1983 年 31 巻 10 号 p. 3377-3384
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe kinetics of oxidation of D-glucose in the presence of glucose oxidase and catalase was studied in a stirred-tank reactor. Experiments were performed using free or immobilized enzyme in 0.1 M acetate buffer solution (pH=5.5) at atmospheric pressure and 25°C. The immobilized enzyme catalyst, which consisted of both glucose oxidase and catalase supported on activated carbon, was prepared by the carbodiimide method. The initial rate of reaction was determined from the amount of oxygen consumed in the absence of external mass transfer resistances. Using free enzyme, the existence of competitive product inhibition by δ-D-gluconolactone was confirmed from Lineweaver-Burk plots, and our results could be well explained by the single substrate mechanism. The effect of mutarotation on the rate of reaction was also taken into account. The activity of immobilized enzyme catalyst was reduced to about 30% of that of the free enzyme. However, the Michaelis and product inhibition constants were not appreciably changed by immobilization. The time-course data were well explained by the proposed kinetic model.抄録全体を表示PDF形式でダウンロード (809K) -
枡井 雅一郎, 大森 秀信, 植田 千裕, 野瀬 浩一, 佐用 博照1983 年 31 巻 10 号 p. 3385-3390
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe paramagnetic species formed by in situ electrochemical oxidation of N-nitroso-2, 2, 6, 6-tetramethylpiperidine (1), N-nitrosodicyclohexylamine (2), and N-nitrosodiisopropylamine (3) in acetonitrile or propionitrile at -30--90°C have been identified as the radical cations, >N+=N-O, derived from the parent nitrosamines by one-electron transfer. The radical cations are σ-radicals isoelectronic with the corresponding iminoxy radicals and show long-range couplings to hydrogen atoms, but the value of hyperfine splitting constant of the nitroso-nitrogen (ca. 45G) is the largest known for a nitrogen atom in an organic molecule. The order to stability of the radical cations is as follows : that derived from 1 > that from 2 > that from 3.抄録全体を表示PDF形式でダウンロード (572K) -
木内 文之, 渋谷 雅明, 木下 武司, 三川 潮1983 年 31 巻 10 号 p. 3391-3396
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーHot aqueous extracts of medicinal plants used in oriental medicine were tested for inhibitory effect on prostaglandin biosynthesis in order to detect biologically active compounds present therein. Of 162 samples tested, 35 showed significant inhibition. Inhibitors of prostaglandin biosynthesis contained in Cyperus rotundus were identified as sesquiterpenes. α-Cyperone, the main inhibitor of C. rotundus, showed competitive-type inhibition with respect to the substrate, arachidonic acid.抄録全体を表示PDF形式でダウンロード (646K) -
山川 浩司, 西谷 潔, 村上 昭弘, 山本 章裕1983 年 31 巻 10 号 p. 3397-3410
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe chemical transformations of α-santonin (1), a C-6 lactonized eudesmanolide, into C-8 lactonized eudesmanolides, i.e., yomogin (2) and four diastereoisomers of dihydrograveolide (36-39), are described. Transposition of 6, 13-olide into 8, 13-olide in eudesmanolides was investigated. Allylic oxidation of the trienone (12) with tert-butyl chromate gave 3, 8-dioxotriene (20) and 3, 6-dioxotriene (22). Reductive lactonization of 20 gave 11α- and 11β-methyl cis-lactones (30 and 31). Yomogin (2) was synthesized from the cis-lactones (32 and 33) by phenylselenenylation and deselenoxylation procedures. Catalytic reduction of 30 and 31 gave diastereoisomers of dihydrograveolide (36-39).抄録全体を表示PDF形式でダウンロード (1339K) -
山川 浩司, 西谷 潔, 村上 昭弘1983 年 31 巻 10 号 p. 3411-3417
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe chemical transformations of α-santonin (1), a C-6 lactonized eudesmanolide, into C-8 lactonized eudesmanolides, telekin (4) and pinnatifidin (5), are described. Desulfurization of the thio-ketal (8), derived from tetrahydroyomogin (7), with Raney Ni gave the 4-ene (10), which was converted into the α-epoxide (12). Ring-opening of the epoxy ring with LiNEt2 afforded the allyl alcohol (13). Phenylselenenylation of 13 gave the selenide (14), and oxidative elimination then gave telekin (4). Bromination of 3-oxoeudesman-8, 13-olide (18) gave the 2α-bromo-3-ketone (19). Reduction of 19 with NaBH4 gave bromohydrins (20 and 21), which were treated with Zn dust to afford the olefin (22). Treatment of 22 with N-bromosuccinimide afforded the 2-hydroxy-3-bromide (24), which was oxidized to give the 2-oxo-3-bromide (25). Dehydrobromination of 25 afforded the 2-oxo-3-ene (26). Pinnatifidin (5) was synthesized from 26 by phenylselenenylation and deselenoxylation procedures.抄録全体を表示PDF形式でダウンロード (715K) -
大石 義孝, 中西 輝雄1983 年 31 巻 10 号 p. 3418-3423
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーEpichlorohydrin [14C-1, 2] (4) was condensed with 2-acetyl-7-hydroxybenzo[b]furan potassium salt (3) to give two radiochemical regio-isomeric 2-acetyl-7-glycidyloxybenzo[b]furans (5a and 5b). The ratio, 5a/5b, was determined to be 5/7 by using 14C-radioisotopic tracer techniques. The present results showed that the reaction proceeds through two different paths in which the phenolate (3) attacks at C-1 of 4 to give 5a and at C-3 to give 5b, the latter path being more favorable than the former.抄録全体を表示PDF形式でダウンロード (671K) -
前田 量三, 大杉 栄一, 藤岡 紀洋, 廣瀬 勝巳1983 年 31 巻 10 号 p. 3424-3445
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーA series of 2-thiazolylamino-, 2-thiazolyloxy- and 2-thiazolylthio-arylacetic acid derivatives was prepared by condensation of thioamides with halo-acetals according to Hantzsch's method, and thioamides having the α-methylarylacetic acid moiety were conveniently obtained from haloaromatic nitro compounds by a combination of known methods. In the model reaction of O-phenyl thiocarbamate (XVIII) with chloro-diethylacetal, isolation of intermediates such as acyclic halo-compound (XIX) and 4-ethoxy-2-phenoxy-2-thiazoline (XX) clarified the reaction path for the formation of 2-phenoxythiazole (XXI). The analgesic and anti-inflammatory effects of the compounds studied were evaluated by using the acetic acid-induced writhing method in mice and the rat carrageenin paw edema method, respectively. 2- [4- (2-Thiazolyloxy) phenyl] propionic acid (XIVa) had the most favorable therapeutic ratio between activity and toxicity (in mice).抄録全体を表示PDF形式でダウンロード (1690K) -
小田 泰子, 佐藤 良博1983 年 31 巻 10 号 p. 3446-3453
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーTo elucidate the stereochemistry of microbial hydrogenation of (+)- and (-)-2'-demethoxydehydrogriseofulvin (1 and 2) by Streptomyces cinereocrocatus NRRL 3443, deuterated substrates (1a, 1b, 2a, and 2b) were synthesized from (+) -griseofulvin (9) and subjected to microbial transformation. The 41.41 MHz 2H nuclear magnetic resonance (NMR) and 400 MHz 1H NMR studies clearly revealed that the microbial hydrogenations of (+)- and (-)-2'-demethoxydehydrogriseofulvin (1 and 2) proceed stereospecifically with an anti-addition of hydrogens at the 2' and 3' positions. Further, the microbial transformation of 1 to (+) -2'-demethoxy-2', 3'-dihydrodehydrogriseofulvin (5) indicates an isomerization by the microorganism of 1 to the enantiomer, (-)-2'-demethoxydehydrogriseofulvin (2), which is further hydrogenated to afford 5.抄録全体を表示PDF形式でダウンロード (793K) -
真野 光彦, 瀬尾 卓司, 今井 欣一1983 年 31 巻 10 号 p. 3454-3459
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe thermal cyclization of 4-amino-6-methylamino- (3) and 4, 6-bis (methylamino) -5-phenylazopyrimidines (4) to adenine (10) and its N6-methyl derivative is described. Compound 3 was synthesized by reaction of phenylazomalononitrile (2) with N-methylformamide and ammonia. Compound 4 was synthesized from 2, formamide, methylamine and its hydrochloride. These compounds were also obtained by methylation of 4, 6-diamino-5-phenylazopyrimidines, followed by rearrangement in methanolic dimethylamine. Heating 4 at 250-260°C afforded 6-methylaminopurine (12) together with a small amount of 8-anilino-6-methylaminopurine (13). Similarly, refluxing 3 in Dowtherm A yielded 10 and 8-anilinoadenine (11).抄録全体を表示PDF形式でダウンロード (697K) -
嶋田 定勝, 前田 博1983 年 31 巻 10 号 p. 3460-3464
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of N-(cyanophenylmethyl)acylamides (1) with olefins (2) in the presence of trifluoroacetic acid gave the corresponding 3-amino-2-phenylpyridines (3) in good yields. Similar reaction of ethyl 2-acylamino-2-cyanoacetates (4) with olefins in the presence of trifluoroacetic acid afforded ethyl 3-aminopyridine-2-carboxylates (5) in a one-pot procedure. The mechanism of the reaction is discussed.抄録全体を表示PDF形式でダウンロード (578K) -
小泉 直之, 池川 信夫1983 年 31 巻 10 号 p. 3465-3470
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe benzoyl group participation in the epoxide ring opening reaction of 26-benzoxy-24, 25-epoxycholesterol derivatives on treatment with perchloric acid in tetrahydrofuran was clearly demonstrated by the transformation of (carbonyl-18O)-3β, 26-dibenzoxy-24, 25-epoxycholest-5-ene into (25-18O)-24, 25, 26-trihydroxycholesterol derivatives.抄録全体を表示PDF形式でダウンロード (609K) -
広井 邦雄, 佐藤 修子, 北山 隆一1983 年 31 巻 10 号 p. 3471-3485
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーSeveral kinds of optically active o-aminoalkylphenols were prepared and used to develop asymmetric synthetic methods for chiral sulfoxides. The reaction of 2, 3-dihydro-1, 2, 3-benzoxathiazine 2-oxides (derived from the o-aminoalkylphenols and thionyl chloride) with phenylmagnesium bromide, followed by treatment with alkyllithium, gave optically active sulfoxides with high enantiospecificity. Among several kinds of optically active o-aminoalkylphenols examined, the readily available aminophenol, (S)-(-)-o-{1-((S)-1-α-naphthylethylamino)ethyl} phenol, was found to be the most efficient and recyclable chiral source for the asymmetric synthesis of sulfoxides.抄録全体を表示PDF形式でダウンロード (1472K) -
渡辺 好章, 真田 修一, 伊田 喜光, 庄司 順三1983 年 31 巻 10 号 p. 3486-3495
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーSeven steroidal glycosides, tentatively named glycosides A, B(1), C(2), D(3), E(4), F(5) and G(6), were isolated from the methanol extract of the subterranean part of Ophiopogon planiscapus NAKAI (Liliaceae). The structures of these glycosides were established as so-called β-sitosterol-β-D-glucopyranoside, diosgenin 3-O-α-L-rhamnopyranoxyl (1→2)-β-D-glucopyranoside (=prosapogenin A of dioscin) (1), diosgenin 3-O-[α-L-rhamnopyranosyl(1→2)]-[β-D-glucopyranosyl-(1→4)]-β-D-glucopyranoside(=deltonin) (2), 26-O-β-D-glucopyranosyl-22-hydroxyfurost-5-ene-3β, 26-diol 3-O-α-L-rhamnopyranosyl(1→2)-β-D-glucopyranoside (3), ruscogenin 1-O-α-L-rhamnopyranosyl(1→2) -4-O-sulfo-α-L-arabinopyranoside (4), 26-O-β-D-glucopyranosyl-22-hydroxyfurost-5-ene-3β, 26-diol 3-O-[α-L-rhamnopyranosyl(1→2)]-[β-D-glucopyranosyl(1→4)]-β-D-glucopyranoside (=22-hydroxyl form of deltoside) (5) and 26-O-β-D-glucopyranosyl-22-hydroxyfurost-5-ene-1β, 3β, 26-triol 1-O-α-L-rhamnopyranosyl(1→2)-4-O-sulfo-α-L-arabinopyranosides (6), respectively. The relationship of steroidal glycosides of Ophiopogon japonicus KER-GAWLER, O. planiscapus NAKAI and Liriope platyphylla WANG et TANG, which are considered to be the plants of origin of the crude drug, Ophiopogonis Tuber, is also discussed. This is believed to be the first report of steroidal glycosides having a sulfate group on the sugar moiety.抄録全体を表示PDF形式でダウンロード (1195K) -
酒向 孫市, 広田 耕作, 牧 敬文1983 年 31 巻 10 号 p. 3496-3502
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThermal reactions of 5-bromouracils 1 with a well-known one-electron donor such as N-methylindole (2) or N-methylphenothiazine (13) result in easy reductive debromination, presumably involving an initial electron transfer process which appears to depend largely upon the nature of the substituents at the N(1)- and C(6)-positions of the uracil ring.抄録全体を表示PDF形式でダウンロード (735K) -
藤井 信孝, 季 惟, 矢島 治明, 森賀 本幸, 水田 和彦1983 年 31 巻 10 号 p. 3503-3514
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーA recently found gastrointestinal hormone, PHI (heptacosapeptide), was synthesized in a different manner from that of Moroder et al. [Z. Naturforsch., 37b, 772 (1982) ]. Our synthesis was carried out by successive azide condensation of six peptide fragments (23-27, 19-22, 15-18, 11-14, 7-10, and 1-6), followed by deprotection with 1 M trifluoromethanesulfonic acid-thioanisole in trifluoroacetic acid. The deprotected peptide was purified by gel-filtration on Sephadex G-25, followed by ion-exchange chromatography on CM-Biogel A and reverse phase high-performance liquid chromatography on μBondapak C18. The homogeneous product thus obtained produced a remarkable decrease in systemic blood pressure in anesthetized rats. In addition, Nα-biotinyl-PHI was synthesized for histochemical receptor-binding studies.抄録全体を表示PDF形式でダウンロード (1226K) -
沢谷 拓治, 木村 道也1983 年 31 巻 10 号 p. 3515-3520
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe autoxidation of bisnorcholanic acid, in an acetate buffer (0.2 M, pH 5.0) solution containing acetone and ferrous ions gave six products, A, B, C, D, E, and F ; product D was the major one. Products A and B were those formed by oxy-functionalization at the side chain with successive decarboxylation, and were identified as 20-oxo-5β-pregnane and 20α-hydroxy-5β-pregnane, respectively. Products C and D were ketones having an oxygen function in ring D and were shown to be 15- and 16-oxo-5β-bisnorcholanic acid, respectively. The minor products E and F were assumed to be hydroxylated derivatives of the substrate, which were formed by the introduction of an oxygen function into ring A, B, or C. No autoxidation occurred when the free carboxyl group of the substrate was protected by methylation or reduced to the alcohol.抄録全体を表示PDF形式でダウンロード (635K) -
藤井 澄三, 斎藤 徹, 中坂 剛志1983 年 31 巻 10 号 p. 3521-3527
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーEthylation of N6-methoxy-3-methyladenine (5) with EtI in AcNMe2 gave the 1-ethylated product 8 (X=I) (21% yield) and the N6-ethylated product 11 (X=ClO4) (33%). The N6-benzyloxy analogue 6, prepared from 3-methyl-6-methylthiopurine (4) and benzyloxyamine, was similarly methylated to produce the 1-methylated product 9 (X=Cl) (34%) as well as the N6-methylated product 12 (X=Cl) (35%). Reduction of N6-methoxy-1, 3-dimethyladeninium iodide (7 : X=I) with NaBH4 afforded the 1, 2-dihydro derivative 14 (92% yield), which reverted to 7 (X=I) on dehydrogenation with I2 in EtOH. On hydrogenation with Raney Ni and H2, 7 (X=I) furnished 14 (26% yield) and the N6-demethoxy derivative 15·HI (17%), while 14 gave 15 on similar reduction. Dehydrogenation of 15 with 2, 3-dichloro-5, 6-dicyano-1, 4-benzoquinone (DDQ) in CHCl3 yielded a crude solid presumed to be the 1, 3-dimethyladeninium salt (18), which readily rearranged into N6, 3-dimethyladenine (16) through the monocycle 17. It has been found that hydrolysis of 7 (X=ClO4) to give the imidazole 13 in H2O at pH 7.72 and 25°C proceeds ca. 270 times as fast as that of the 3, 9-dimethyl analogue 19 to give the monocycle 20.抄録全体を表示PDF形式でダウンロード (830K) -
後藤 玲子, 森崎 益雄, 池川 信夫1983 年 31 巻 10 号 p. 3528-3533
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリー(20S)-Cholest-5-en-3β-ol(20-isocholesterol) was chemically prepared from bisnorcholenic acid. Incubation of cytochrome P-450scc with 20-isocholesterol produced no pregnenolone. 20-Isocholesterol did not satisfy the silkworm sterol requirement. Liposomes containing cholesterol or 20-isocholesterol behaved similarly when examined either by differential scanning calorimetry, or for permeation of carboxyfluorescein from the liposomes.抄録全体を表示PDF形式でダウンロード (596K) -
尾能 満智子, 田中 比奈子, 早川 和秀, 田村 真造1983 年 31 巻 10 号 p. 3534-3543
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe alkaline hydrolyses of N1-benzoyl-N1, N2-diarylacetamidine (V) and N1-tosyl-N1, N2-diarylacetamidine (IX) were examined. In the hydrolysis of V, hydroxide ion attacked the amide carbonyl carbon to form N1, N2-diarylacetamidine and benzoic acid. In the hydrolysis of IX, hydroxide ion attacked the amidine carbon, and elimination of the N-tosylarylamino group and arylimino group proceeded in parallel, with that of the latter predominating. The alcoholysis reaction of V proceeded without any added catalyst, in contrast to the case of 1- (N-benzoylarylamino) -3-arylimino-1-propene. A unique peak corresponding to the loss of 64 mass units (sulfur dioxide) was observed in the mass spectrum of IX.抄録全体を表示PDF形式でダウンロード (921K) -
山川 浩司, 佐藤 毅, 滝田 敏, 飯田 敏明, 岩崎 正志1983 年 31 巻 10 号 p. 3544-3552
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe syntheses of several 10β-hydroxyfuranoeremophilane derivatives, (±)-10β-hydroxyfuranoeremophilane-3, 6-dione (3), (±)-10β-hydroxyfuranoeremophilan-6-one (4), and (±)-10β-hydroxy-6β-isobutyryloxyfuranoeremophilan-9-one (5), are described. The key step in these syntheses is the angular hydroxylation of 10βH-furanoeremophilane-6, 9-dione (6) using benzeneseleninic anhydride. Reduction of the 10β-hydroxy-6, 9-dione (7) with NaBH4 or ZnNH4OH gave the 9α- or 9β-hydroxy compounds (9a and 10), respectively. The stereochemistries of the diols (9a and 10) were confirmed by the chemical conversion of 9a to the known compound 17. Treatment of 9a and 10 with methanesulfonyl chloride-Et3N afforded the 9β, 10β-epoxide (18). Ring-opening of 18 with NaBH4 gave the 10β-hydroxy compound (21). Deacetalization of 21 with aq. acetic acid afforded (±)-3. Desulfurization of the 3, 3-dithioacetal (24) which was derived from 21 with Raney Ni gave (±)-4. The enone (27a) was treated with isobutyric anhydride followed by catalytic reduction to afford 28b as a major product. Hydroxylation of 28 with benzeneseleninic anhydride in the presence of NaH in chlorobenzene afforded the 10β- and 10α-hydroxy compounds (29a and 29b). Desulfurization of the 3, 3-dithioacetal of 30a which was derived from 29a with Raney Ni gave (±)-5.抄録全体を表示PDF形式でダウンロード (978K) -
林 公明, 沼波 憲一, 坂井 和夫, 尾崎 泰彦, 加藤 錠治, 木梨 計三, 米田 直人1983 年 31 巻 10 号 p. 3553-3561
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリー(3S)-2-[N-Substituted N-(2-carboxyethyl)carbamoyl]-1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylic acid derivatives (V) were synthesized by condensation of (3S)-1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylates (III), 3-alkylaminopropionates (II), and phosgene, followed by cleavage of ester groups. The in vitro angiotensin converting enzyme (ACE) inhibitory activities of these dicarboxylic acid derivatives (V) were evaluated. Among them, N-ethyl (13) and N-isopropyl (14) derivatives showed high inhibitory activities with IC50 values of 1.1×10-8 and 7.7×10-8M, respectively. These compounds showed only weak inhibition of the pressor response to angiotensin I after oral administration in normotensive rats. Thus, in order to derive orally active inhibitors, the ester derivatives (IV, VI, and VII) were prepared as prodrugs of the dicarboxylic acids (V). Of these esters, the monoester compounds (VI) having the ester function at the side chain were found to be orally active. In particular, (3S)-2-[N-ethyl-N-(2-butoxycarbonylethyl)carbamoyl]-1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylic acid (20) inhibited the pressor response to angiotensin I by up to 82% at an oral dose of 1.0 mg/kg.抄録全体を表示PDF形式でダウンロード (831K) -
/ 坂東 英雄, 網谷 孝, TAKASHI AMIYA1983 年 31 巻 10 号 p. 3562-3565
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーTwo new piperidine alkaloids, pipernonaline and piperundecalidine, were isolated from fruits of Piper longum L. (Piperaceae). Their structures were determined to be (2E, 8E)-N-[9-(3, 4-methylenedioxyphenyl)-2, 8-nonadienoyl]piperidine and (2E, 4E, 10E)-N-[11-(3, 4-methylenedioxyphenyl)-2, 4, 10-undecatrienoyl]piperidine, respectively, on the basis of spectral data.抄録全体を表示PDF形式でダウンロード (475K) -
太田 美矢子, 徳永 裕司, 木村 俊夫, 佐藤 浩, 川村 次良1983 年 31 巻 10 号 p. 3566-3570
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーA reversed-phase high-performance liquid chromatographic (RP-HPLC) method for the separation of bovine, porcine, ovine and equine insulins has been investigated. The complete chromatographic separation of these four insulins was achieved on a column of LiChrosorb RP-18 (5μm) with a mixture of acetonitrile and 5mM tartrate buffer (pH 3.0) containing sodium sulfate as the mobile phase at 40°C. The capacity factors of the four insulins were greatly affected by the concentrations of acetonitrile and sodium sulfate in the mobile phase and by the column temperature. Careful preparation of the mobile phase and a constant column temperature are essential for the reproducible and complete separation of insulins by this RP-HPLC method.抄録全体を表示PDF形式でダウンロード (528K) -
広島 修, 池谷 理, 内藤 俊彦, 楠部 健一, 大前 雅彦, 河部 靖, 石川 靖二, 星田 晴彦, 倉橋 辰雄1983 年 31 巻 10 号 p. 3571-3578
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe fundamental characteristics of a twin electrochemical detector were evaluated to investigate its suitability as a detector for high-performance liquid chromatography. This novel detector was proved to have the following advantages compared to the conventional three-electrode detector. 1) Simultaneous determination of reduced and oxidized species is possible, 2) the stability of the electrode is improved by applying a larger potential to the other electrode, 3) the specificity of detection is improved by the re-electrolysis at the second electrode of the reaction product produced at the first electrode, and 4) specific detection of the post-discharging materials and sensitive detection are possible by using appropriate operating circuits.抄録全体を表示PDF形式でダウンロード (651K) -
岩井 広行, 石原 文子, 秋浜 澄行1983 年 31 巻 10 号 p. 3579-3582
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe oxidation of homovanillic acid by peroxidase in the presence of hydrogen peroxide is stimulated by various compounds. Among the compounds tested, o-dianisidine was found to stimulate the oxidation of homovanillic acid strongly. A rapid and highly sensitive method for the fluorometric rate assay of peroxidase using o-dianisidine as an oxidative stimulator in the homovanillic acid-hydrogen peroxide system was established. By this method, it is possible to determine peroxidase activity in the range of 0.5-18 mU/ml.抄録全体を表示PDF形式でダウンロード (421K) -
南原 利夫, 大久保 正, 八巻 輝子, 島田 和武1983 年 31 巻 10 号 p. 3583-3588
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe preparation and antigenic properties of estradiol 3-glucuronide-bovine serum albumin conjugate in which the hapten is linked to the carrier protein through an (O-carboxymethyl) oxime bridge at the C-6 position on the steroid nucleus, are described. Antiserum elicited in the rabbit by the immunogen possessed high affinity and specificity to estradiol 3-glucuronide, exhibiting hardly any cross-reactivities with other estrogen conjugates except for estrone 3-glucuronide (18.66%) and no cross-reactions with free estrogens and other related steroids. This antiserum was purified by affinity chromatography on estrone 3-glucuronide-aminoethyl cellulose conjugate. The purified antiserum exhibited no cross-reaction with estrone 3-glucuronide. A direct radioimmunoassay method for urinary estradiol 3-glucuronide was developed by using the purified antiserum. The values obtained with the purified antiserum were somewhat lower than those with the native one. The within- and between-assay variations were 3.32 and 4.35%, respectively. The values obtained by the present method correlated closely with those obtained by the established indirect radioimmunoassay (RIA) method.抄録全体を表示PDF形式でダウンロード (678K) -
楠部 健一, 阿部 皓一, 広島 修, 石黒 義信, 石川 靖二, 星田 晴彦1983 年 31 巻 10 号 p. 3589-3594
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーA novel technique using on-line electrochemical derivatization of thiamine is described which can enhance considerably both the sensitivity and specificity of detection. Material injected is electrolyzed in a flow electrolytic cell which may induce a reaction yielding highly fluorescent or ultraviolet (UV) -absorbing products. The electrolyzed eluent then passes into a suitable detector. An example of the use of this technique is in the detection of thiamine which was found to form a highly fluorescent product, thiochrome, by electrochemical oxidation in the presence of sodium hydroxide. In the present investigation, we used such a flow injection method to determine thiamine content specifically in some pharmaceuticals.抄録全体を表示PDF形式でダウンロード (526K) -
細田 宏, 小林 典裕, 河本 裕子, 南原 利夫1983 年 31 巻 10 号 p. 3595-3600
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーIn order to develop an 11-deoxycortisol enzyme immunoassay applicable to metyrapone tests, the specificity obtainable with various assay systems has been investigated. Four 11-deoxycortisol derivatives possessing different bridges at C-4 were covalently linked to β-galactosidase to give enzyme-labeled antigens. The anti-11-deoxycortisol antisera used were those elicited in rabbits by immunization with the conjugates of these haptenic derivatives with bovine serum albumin. Enzyme immunoassays were carried out with the homologous and bridge heterologous combinations between antiserum and enzyme-labeled steroid. The specificity of these assay systems was assessed by measuring the amount of 11-deoxycortisol in human plasma specimens, and by comparison of the results with those of radioimmunoassay. The assay employing the antiserum and enzyme-labeled antigen which were prepared by the use of 4-(carboxymethylthio)-11-deoxycortisol was found to be relatively specific. The cross-reactivities in this assay were tested with six kinds of closely related steroids. The selective blocking of less specific antibodies present in the antiserum was also examined. It was found that the addition of cortisol to the antiserum resulted in improvement of the specificity. The enzyme immunoassay thus developed was reasonably specific and sensitive.抄録全体を表示PDF形式でダウンロード (679K) -
神力 就子, 石崎 紘三, 三浦 一伸, 上田 亨, 原田 文夫1983 年 31 巻 10 号 p. 3601-3608
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe degradation of mouse [32P]proline transfer ribonucleic acid (tRNA) and [32P]isoleucine tRNA with ozone (concentration in inlet gas, 0.1 mg/l) was examined in aqueous solution (reaction time, 0-32 min) and sequence analysis of the products was performed by digestion with ribonuclease A or T1 according to Sanger's method. The guanine moieties in the nucleobases were preferentially attacked by ozone and the cleavage of polynucleotidic linkages did not occur during the ozonization. Proline tRNA was more degradable than isoleucine tRNA, probably as a result of differences in the locations of the guanine residues in their higher-order structures. The consecutive guanine residues in the anticodon and dihydrouracil (D) regions of proline tRNA were most susceptible to degradation with ozone. In the case of isoleucine tRNA, which does not have the conseutive guanine residues in the anticodon region, those in the D-loop, small (S) loop and the common stem were degraded. Therefore ozone seems to start reacting with the guanine moieties located in the most exposed regions of the higher-order structure of tRNA.抄録全体を表示PDF形式でダウンロード (913K) -
亀井 敏夫, 浅野 和子, 近藤 久雄, 松崎 明紀, 中村 昭四郎1983 年 31 巻 10 号 p. 3609-3616
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe properties of L-glutamate oxidase, a novel L-glutamic acid oxidizing enzyme from Streptomyces violascens H82-N-SY7 were examined. The enzyme showed absorption maxima at 280, 390 and 470 nm and a marked shoulder at 490 nm, and contained 1 mol of flavin-adenine dinucleotide (FAD) per mol of enzyme. Enzyme activity was inhibited by Ag+, Hg2+, p-chloromercuribenzoate (PCMB) and N-bromosuccinimide. The enzyme catalyzed the oxidation of L-glutamic acid using molecular oxygen as a primary electron acceptor and produced α-ketoglutaric acid, NH3 and hydrogen peroxide according to the following schema : L-glutamic acid+H2O+O2→α-ketoglutaric acid+NH3+H2O2. L-Glutamate oxidase was used in a specific and sensitive determination procedure for L-glutamic acid.抄録全体を表示PDF形式でダウンロード (724K) -
Identification of a Serum Glycoprotein Whose Content is Increased in PSK-Treated Mice as Haptoglobin満野 徹, 設楽 研也, 児島 英介, 大沢 利昭1983 年 31 巻 10 号 p. 3617-3624
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーA serum glycoprotein whose content is increased in mice by the administration of an antitumor agent, PSK, and which migrates to the so-called LC region on polyacrylamide gradient gel electrophoresis, was purified by repeated ion-exchange column chromatography on DEAE-Sephadex A-50, chromatofocusing and gel filtration. The purified protein was identified as mouse haptoglobin, since its chemical composition, isoelectric point (4.1), molecular weight (94000) and subunit structure were found to be very similar to those of human haptoglobin. Furthermore, the purified protein formed a complex with hemoglobin and increased the peroxidase activity of hemoglobin.抄録全体を表示PDF形式でダウンロード (924K) -
清水 譲, 小林 優1983 年 31 巻 10 号 p. 3625-3631
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーIn order to explore the origin of the potent neurotoxin tetrodotoxin, feeding experiments were carried out using [2-14C]-acetate, [guanido-14C]-arginine, [ureido-14C]-citrulline and [14C (U)]-glucose on the newts Taricha torosa and Taricha granulosa. The precursors were administered by injection, by oral feeding, or by soaking the newts in a bath of water containing the radioactive precursors. None of these feeding experiments resulted in the incorporation of radioactivity into tetrodotoxin, though common metabolites such as cholesterol, amines, amino acids, and macromolecular compounds were significantly labeled. The toxicities of T. granulosa and T. torosa used for the experiment were found to be higher than those previously reported. They retained a high level of toxicity during their captivity, yet they were found to continuously release small amounts of toxins (2.5% of the total toxins in one year). When subjected to an electric shock, the newts released significant amounts of toxin.抄録全体を表示PDF形式でダウンロード (761K) -
山村 恵子, 中尾 誠, 山田 潤一郎, 四柳 智久1983 年 31 巻 10 号 p. 3632-3636
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーFor the purpose of investigating of its suitability for topical application, the stability of sisomicin incorporated in hydrophilic petrolatum was investigated under various storage conditions by high-performance liquid chromatography. Sisomicin was extracted from the oleaginous vehicle, which was kept in a liquid state by adding liquid paraffin, using pH 6.5 phosphate buffer. An appropriate retention behavior of the antibiotic is obtained on a μBondapak-C18 column with a mobile phase of 2.0% (w/v) sodium sulfate-0.005 M sodium 1-pentanesulfate (detection at 214 nm). The degradation of sisomicin follows first-order kinetics with regard to the remaining antibiotic in aqueous solution : the apparent first-order rate constants are 2.63×10-3 d-1 at 5°C and 1.70×10-2 d-1 at 25°C. When incorporated in hydrophilic petrolatum, the antibiotic is 5 to 7 times more stable than in an aqueous medium. This is due to the reduction of its surface oxidation. Accordingly, the ointment is therapeutically effective for at least 3 months when preserved under shielding from light at 5°C.抄録全体を表示PDF形式でダウンロード (636K) -
上釜 兼人, 上村 雄司, 入江 徹美, 小田切 優樹1983 年 31 巻 10 号 p. 3637-3643
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe interfacial transfer and absorption behavior of drugs following dissolution from inclusion complexes was analyzed by the use of in vitro and in situ models (S-Lw-Lo and S-Lw-in situ). The experiments were carried out using 1 : 1 complexes of β-cyclodextrin (β-CyD) with some barbiturates and p-aminobenzoic acid esters as test compounds. Taking into account the dissolution equilibrium of complexes in the dissolution medium, the drug appearance in the organic phase of the S-Lw-Lo model and the amount of drug absorbed in the S-Lw-in situ model were analyzed in relation to time. The factors affecting the interfacial transfer and in situ absorption behavior of the complexes are discussed. The results indicate that the two experimental models are applicable to β-CyD complexes, and may be suitable for the evaluation of their oral bioavailability.抄録全体を表示PDF形式でダウンロード (642K) -
堀 了平, 岩川 精吾, 鍵本 順子, 大倉 節子, 奥村 勝彦1983 年 31 巻 10 号 p. 3644-3648
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーExperimental utilization of isolated vascularly perfused rat stomach with retention of the exocrine response to various stimulants was studied. By the inclusion of bovine erythrocytes in the vascular perfusate and by the use of luminal perfusate possessing a suitable buffer capacity, it was found that acid secretion was significantly stimulated by the perfusion of histamine, pilocarpine, cyclic adenosine monophosphate (AMP), dibutyryl cyclic AMP or theophylline. In addition, cimetidine, a histamine H2-receptor antagonist, inhibited histamine-induced acid secretion in a reversible manner. Although tetragastrin stimulated acid secretion in immature rat or guinea pig stomach, it caused little secretory response in adult rat stomach. On the addition of pepstatin, a pepsin inhibitor, to the vascular perfusate, an acid secretion induced by tetragastrin in adult rat stomach was observed. These findings indicate that some changes in gastrin receptors may develop during the maturation process and that gastrin-induced acid secretion is easily altered by peptic activity in the gastric glands of the perfused stomach. The proposed perfusion system should be useful for studying drug distribution, metabolism and action in the stomach.抄録全体を表示PDF形式でダウンロード (550K) -
/ 岡本 喜久子, 千原 薫, 城谷 憲一, 津田 泰之, 鈴木 悦子, 関口 慶二, KEIJI SEKIGUCHI1983 年 31 巻 10 号 p. 3649-3655
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーAdduct formation with ammonia (NH3) was confirmed to occur with four steroids (cortisone acetate, hydrocortisone acetate, prednisolone, and prednisone). The thermal, physico-chemical, and micromeritic properties of these adducts were investigated by differential scanning calorimetry, thermogravimetry, thermomicroscopy, infrared spectroscopy, X-ray powder diffractometry, electron microscopy, and BET gas adsorption analysis. From the results of thermogravimetry, the combining ratios of the adducts (steroid : NH3) were determined to be 1 : 1.13 and 1 : 0.95 for cortisone acetate and hydrocortisone acetate, respectively ; however, in the cases of prednisolone and prednisone, one molecue of the steroid combined with 0.5-1 or 1-2 molecules of NH3, respectively. The formation of adducts having nonstoichiometric ratios may be due to the fact that the architecture of molecules rather than their chemical affinity may play an important role in adduct formation. Elimination of NH3 from adducts proceeded completely at room temperature and under the reduced pressure to yield ultrafine particles of the original steroids.抄録全体を表示PDF形式でダウンロード (1026K) -
田中 頼久, 西川 優子, 林 了三1983 年 31 巻 10 号 p. 3656-3664
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーUrinary metabolites of loxoprofen-14C sodium were determined in rats, mice, dogs and monkeys after oral administration of the drug. In all these animal species, the cyclopentanone moiety of loxoprofen was predominantly reduced to trans-OH (an active principle), together with cis-OH (minor product). The monohydroxy metabolites were further hydroxylated in rats to the diols (M-4, M-5 and M-6), which were excreted in urine as the main metabolites. Mice excreted the monohydroxy metabolites mainly as their free forms. In dogs, the monohydroxy metabolites were conjugated with taurine and glucuronic acid, and monkeys furnished the ester glucuronides of the monohydroxy metabolites. Thus, species differences were observed both in the hydroxylation and in the conjugation reactions of the monohydroxy metabolites produced by the reduction of loxoprofen.抄録全体を表示PDF形式でダウンロード (917K) -
鍵本 順子, 小長井 規世子, 木村 良平, 村田 敏郎1983 年 31 巻 10 号 p. 3665-3670
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーIncubation of a heavy lysosome-containing (3500×g) fraction from rat liver with ascorbic acid resulted in a marked increase in the formation of lipid peroxides, and a concomitant increase in the release of two marker enzymes, acid phosphatase and aryl sulfatase, from lysosomes. These simultaneous increases in the lipid peroxidation and the lysosomal enzyme release were completely inhibited by adding ethylenediamine tetraacetic acid, indicating that the ascorbic acid-induced lipid peroxidation is responsible for the labilization of lysosomes. Sodium copper chlorophyllin (Cu-Chl-Na) caused a concentration-dependent inhibition of both the lipid peroxidation and the release of marker enzymes which were stimulated by ascorbic acid, and the dose-inhibition curves showed nearly the same pattern. Cu-Chl-Na also prevented the stimulation of lipid peroxidation and release of aryl sulfatase by ferrous ion. These findings indicate that Cu-Chl-Na has the ability to protect liver lysosomes from peroxidative damage, and this effect is ascribed to an inhibition of lipid peroxidation. Cu-Chl-Na also moderately inhibited the release of two marker enzymes from lysosomes in 0.25 and 0.18 M sucrose media, suggesting a direct stabilizing effect of Cu-Chl-Na on the lysosomal membrane.抄録全体を表示PDF形式でダウンロード (657K) -
田島 和男, 山本 健次, 水谷 民雄1983 年 31 巻 10 号 p. 3671-3677
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーRats which had received butylated hydroxytoluene (BHT) excreted S- (3, 5-di-tert-butyl-4-hydroxybenzyl) glutathione (BHT-glutathione) and 3, 5-di-tert-butylhydroquinone (BHQ) glucuronide in the bile. After being separated by high-performance liquid chromatography, the glutathione conjugate was identified by 13C-nuclear magnetic resonance and field desorption mass spectrometry ; the glucuronide was identified by gas chromatography-mass spectrometry. The structures of BHT-glutathione and BHQ glucuronide were further confirmed by comparison with synthetic samples. The excretion rates of BHT-glutathione and BHQ glucuronide in rat bile were 3.5 and 1.6%, respectively, of the dose in 24h after intraperitoneal administration of BHT at a dose of 400 mg/kg. The occurrence of BHT-glutathione suggests that 2, 6-di-tert-butyl-4-methylene-2, 5-cyclohexadienone, a toxic metabolite of BHT, is detoxified by glutathione conjugation.抄録全体を表示PDF形式でダウンロード (687K) -
山本 都, 山田 隆, 谷村 顕雄1983 年 31 巻 10 号 p. 3678-3683
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーEthylenethiourea (ETU), a degradation and metabolic product of ethylenebisdithiocarbamate fungicides, was nitrosated by NaNO2 to form N-nitrosoethylenethiourea (NETU). ETU was nitrosated much more rapidly than morpholine and methylurea, which are easily nitrosatable compounds, and NETU formation increased with lowering of the pH. NETU was most unstable around pH 10 and was rather stable in strongly alkaline media above pH 12. The main decomposition reaction of NETU in acidic media was denitrosation. Transnitrosation by NETU to secondary amines gave high yields of nitrosamines at pH 3 and even at pH 5.抄録全体を表示PDF形式でダウンロード (716K) -
栗田 城治, 円角 美智子, 土屋 隆1983 年 31 巻 10 号 p. 3684-3690
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーTreatment of the N-unsubstituted 3-methyl-1H-1, 2-thieno[2, 3-c]diazepine (3) with ethyl chloroformate, acetyl chloride, or benzoyl chloride in benzene resulted in ring-conversion to give the corresponding 3-acyl-3H-1, 3-thieno[2, 3-d]diazepines (4), whereas similar treatment of the N-substituted thieno[2, 3-c]diazepine (6) gave the exo-methylene compound (7) and treatment of the fully unsubstituted thieno[2, 3-c]diazepine (8) gave the thieno[2, 3-b]pyridine derivatives (9) and (10). On the other hand, the N-unsubstituted 3-methyl-1H-1, 2-benzo[c]diazepines (16), upon treatment with ethyl chloroformate in benzene, gave the exo-methylene compounds (17), and in the case of the diazepines (16b, c) having an electron-donating group in the 7-position, the 3-acyl-3H-1, 3-benzo[d]diazepines (19) were also formed. The mechanisms of these acylations are discussed.抄録全体を表示PDF形式でダウンロード (743K) -
小谷 功, 谷澤 久之, 滝野 吉雄1983 年 31 巻 10 号 p. 3691-3697
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe decomposition of ginsenoside-Rg1 and ginsenoside-Rb1 in the rat stomach and large intestine after oral administration was investigated. In the stomach, a part of ginsenoside-Rg1 was decomposed and six decomposition products were observed on a reversed phase thin-layer chromatogram (TLC). These six compounds were identical with those which were obtained on hydrolysis of ginsenoside-Rg1 under mild acidic conditions (with 0.1 N HCl, at 37°C). On the other hand, an unidentified deomposition product of ginsenoside-Rb1 was observed on the TLC of the stomach sample after the oral administration of Rb1 to rats. The product was different from the decomposition product formed by the hydrolysis of Rb1 under mild acidic conditions. In the large intestine, Rg1 was decomposed to ginsenoside-Rh1 and ginsenoside-F1 by tetracycline-susceptible bacteria and tetracycline-resistant bacteria, respectively. Ginsenoside-Rb1 was decomposed to ginsenoside-Rd and two unidentified products by enteric enzyme and tetracyclineresistant bacteria, respectively.抄録全体を表示PDF形式でダウンロード (638K) -
三村 邦雄, 馬場 茂雄1983 年 31 巻 10 号 p. 3698-3706
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーStudies on the percutaneous absorption, metabolism and excretion of paeonol (2-hydroxy-4-methoxyacetophenone, I) were carried out by using the stable isotope (SI) method, which is applicable to man. Radioactive tracer experiments in rats were also performed in order to evaluate the SI tracer technique. Hydrophilic ointment or absorptive ointment containing 5% I was topically applied under an occlusive dressing to man and rat for 6, 12 and 24 h. The amounts of metabolites (2, 5-dihydroxy-4-methoxyacetophenone II, resacetophenone III, and unchanged substrate I) excreted in the urine were determined by selected ion monitoring assay using I [methoxy-d3], II [methoxy-d3] and III [acetyl-13C2] as internal standards. After topical application of hydrophilic ointment for 6 h in man, the amounts of I, II and III in 0-24-h urine were 3.35, 16.28 and 5.17% of the applied dose, respectively. Urinary excretion of I metabolites continued for 6 d from the time of application, but the total amount of metabolites excreted in 0-24 h was as much as 89% of that excreted in 0-144 h. The results indicate that the SI tracer technique described here has sufficient sensitivity and repeatability. Paeonol is easily absorbed through the skin, and the metabolites are excreted rapidly in urine.抄録全体を表示PDF形式でダウンロード (861K) -
宮崎 正三, 竹内 繁美, 坂本 美恵子, 高田 昌彦1983 年 31 巻 10 号 p. 3707-3713
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーEthylene-vinyl alcohol (EVAl) copolymer was evaluated as a carrier for controlled release of 5-fluorouracil (5-FU). In order to study the effect of comonomer ratio modifications on the drug release kinetics, the release of 5-FU dispersed in polymer matrices composed of different ratios of ethylene and vinyl alcohol was investigated. The ethylene content of EVAl copolymer was varied from 32 to 60 mol%. An increase in ethylene comonomer content decreased the drug release from the polymer matrix. The release rate could be controlled by modifying the ethylene/vinyl alcohol ratios in the polymer matrices. Fabrication parameters such as drug content and surface area of matrices also affected the release kinetics. The release rates were shown to be proportional to release media temperature, but independent of the pH. Matrices composed of EVAl copolymer appeared to be stable on long-term storage with respect to release rate and could be useful vehicles for the controlled release of hydrophilic drugs.抄録全体を表示PDF形式でダウンロード (701K) -
末松 和美, 中村 克之, 武田 順一1983 年 31 巻 10 号 p. 3714-3717
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーCondensation of 2, 2-bis[4-(4-aminophenoxy)phenyl]propane and terephthalaldehyde in dilute solution was found to give a highly crystalline powder in 5-90% yield. The product had remarkable similarities to the linear polymer having the same repeating unit. But its nonmacromolecular character was elucidated by gel permeation chromatogram and field desorption mass analyses. A dimeric ring structure is proposed.抄録全体を表示PDF形式でダウンロード (444K) -
木邑 道夫, 岡林 一蔵, 安岡 則武1983 年 31 巻 10 号 p. 3718-3723
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーThe crystal and molecular structure of 1, 2-dihydro-5-methyl-2-phenyl-4- (9H-thioxanthen-9-yl) -3H-pyrazol-3-one was examined by the X-ray diffraction method to establish the predominant tautomeric form (3b) due to the pyrazol-3-one ring in the solid state. The title compound, C23H18N2OS, crystallizes in space group Cc with lattice parameters a=17.675 (8), b=12.421 (3), c=11.374 (7) Å, β=132.57 (3)°, and Z=4. In crystals, molecules of 3b are linked by an intermolecular hydrogen bond between the NH and C=O groups.抄録全体を表示PDF形式でダウンロード (534K) -
上條 哲聖, 山本 亮治, 原田 弘, 飯塚 欣二1983 年 31 巻 10 号 p. 3724-3727
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーAcylation of alcohols with acid anhydrides or acid halides could be considerably accelerated by adding 1-substituted imidazoles as catalysts. The acylation with acid halides required the addition of triethylamine to capture the resulting acid. 1-Isopropyl-5-methylimidazole and 1-(4-methoxybenzyl)-5-methylimidazole showed higher catalytic activities than 4-dimethylaminopyridine (DMAP) for acylation of primary and secondary alcohols.抄録全体を表示PDF形式でダウンロード (443K) -
森田 光, 田中 雅明, 高木 要1983 年 31 巻 10 号 p. 3728-3731
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリー6-(2-Hydroxyphenyl)-2-thiouracil (2a) and its 5-chloro and 5-bromo derivatives (2b, c) were synthesized by the reactions of 4-methoxycoumarin (1a) and 3-chloro- and 3-bromo-4-methoxycoumarins (1b, c), respectively, with thiourea in the presence of sodium ethoxide. In these reactions, compound 1c gave not only the pyrimidine 2c, but also the Perkin rearrangement product : N-(3-ethoxybenzofuran-2-carbonyl)thiourea (3). 2-Thiouracils 2a-c were converted to the uracil derivatives (6a, b). Reactions of 2a-c with some cyclic amines and the methylation of 2b, c with methyl iodide were also examined.抄録全体を表示PDF形式でダウンロード (495K) -
早川 江, 岡田 栄二, 東久世 秀昭, 川本 健志1983 年 31 巻 10 号 p. 3732-3735
発行日: 1983/10/25
公開日: 2008/03/31
ジャーナル フリーAn improved reversed-phase high-performance liquid chromatographic method is proposed for the determination of lysozyme. The protein was separated on a short column (4mm i.d.×50mm) packed with octadecylsilane-bonded silica gel (Nucleosil 10C18) by linear gradient elution using 0.1 M sodium phosphate buffer, pH 2.0 (solvent A) and a mixture of isopropanol, ethylene glycol and solvent A (3 : 1 : 1), apparent pH 2.0 (solvent B). Monitoring was done with a ultraviolet detector. Under the elution conditions, lysozyme was recovered from the column in a high yield (97%). This method was found to be applicable to the determination of lysozyme chloride in antiphlogistics.抄録全体を表示PDF形式でダウンロード (430K)