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掛見 喜一郎, 有田 隆一, 北沢 式文, 河村 光雄, 武仲 宏
1967 年 15 巻 12 号 p.
1819-1827
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Three series of PAS derivatives, alkyl, ω-hydroxyalkyl, and ω-phenylalkyl esters, were synthesized systematically and their evaluations were made with testing their tuberculostatic activities and with measuring their physico-chemical characteristics, such as partition coefficients and protein binding ratio that might considerably influence biological effects in animal body. It is recognized that these derivatives may extensively improve the defects of the parent compound. It is also demonstrated that the substituents on the end of the alkyl chain and the length of the alkyl chain of these compounds considerably influence on their antitubercular activities and physico-chemical properties.
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掛見 喜一郎, 有田 隆一, 北沢 式文, 佐川 良寿
1967 年 15 巻 12 号 p.
1828-1840
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Nine series of ω-substituted PAS alkyl esters, namely, ω-chloroalkyl, ω-aminoalkyl, ω-diethylaminoalkyl, ω-phenylethylaminoalkyl, ω-morpholinoalkyl, ω-pyrrolidinylalkyl, ω-piperidinoalkyl p-aminosalicylates and alkylene bis-p-aminosalicylates in which the alkyl length varied from ethyl to decyl were synthesized and their evaluations were made with testing their tuberculostatic activities and with measuring their physicochemical properties such as partition coefficients and degrees of protein binding that might considerably influence biological effects of these substances when administered in animal body. These synthesized derivatives have activities as same extent as the parent compound and are more lipid soluble and some of them are less protein bound than PAS. From these observations, it is considered that some of the defects of the parent compound are improved by these chemical modifications. Relationship between structures and these characteristics are also revealed.
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小澤 光, 百瀬 和享, 町田 征子
1967 年 15 巻 12 号 p.
1841-1846
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Dihydroxythymoquinone (DTQ) showed a marked inhibitory action on State-3 respiration of rat liver mitochondria with succinate, whereas, State-4 respiration was not inhibited. This inhibition was neither released by 2, 4-dinitrophenol nor other uncoupling agents. Completely DTQ inhibited oxidation of succinate by electron transport particles but the rate of inhibition was less than that of State-3 respiration by intact mitochondria. Reduction of cytochrome c by mitochondria with succinate was also inhibited. Succinate dehydrogenase was stimulated by DTQ.
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清水 文治, 浅井 素次, 西村 卓三
1967 年 15 巻 12 号 p.
1847-1855
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
A convenient synthetic procedure of pyrimidine and purine nucleotides was described. The fusion of phosphorylated acylhalogenoses with trimethylsilylpyrimidines or-purines and then removal of the protecting groups gave several nucleotides in good yields. The structural confirmation of the nucleotides thus obtained was achieved by chromatographic and spectral analyses, as well as comparison with the authentic samples prepared by the known methods.
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浅井 素次, 宮木 美知子, 清水 文治
1967 年 15 巻 12 号 p.
1856-1862
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
A direct synthetic method of purine and pyrimidine nucleotides has been described. Condensation of III with 2, 3-di-O-benzoyl-5-diphenylphosphoryl-D-ribofuranosyl bromide in dimethylformamide at 40∼50°, followed by removal of the protecting groups gave AMP. Several other purine and pyrimidine nucleotides were also obtained by the same method mentioned above. In those cases, nitromethane, dimethylsulfoxide, acetonitrile and dimethylacetamide were effective for the reaction as solvents.
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浅井 素次, 稗田 治清, 清水 文治
1967 年 15 巻 12 号 p.
1863-1870
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
The chloromercuri salt of 6-benzamidopurine was condensed with 2, 3, 5-tri-O-benzoyl-DL-ribofuranosyl chloride, then the protecting groups removed, β-DL-adenosine was produced. β-DL-Adenosine was treated with nitrous acid to afford DL-inosine. β-DL-AMP was obtained by phosphorylation of β-DL-adenosine with phenylphosphorodichloridate. In a similar manner β-DL-IMP was obtained starting from β-DL-inosine. Attempts were made with success to obtain L-adenosine by incubation of DL-adenosine with a bacterial cell suspension (the strain used was PS-264, an unidentified stock culture of our laboratories). The incubation for 2∼3 days resulted in complete deamination and hydrolysis of D-adenosine whereas about 50% of L-adenosine remained unattacked and the rest was deaminated to give the corresponding L-inosine. On the other hand, when DL-AMP was incubated with a snake venom obtained from Trimeresurus flavoviridis, only D-antipode was dephosphorylated to D-adenosine and L-AMP left unchanged. L-AMP was separated from D-adenosine by ion exchange chromatography. L-IMP was also obtained from DL-IMP by the same method.
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小林 五郎, 古川 淳, 松田 芳郎, 鷲田 侑子
1967 年 15 巻 12 号 p.
1871-1874
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Several 2-methylthio-2-(3-indolyl) acrylic acid derivatives (III) were prepared by reacting indolylmagnesium bromides (I) with ketenethioacetals (II).
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小澤 光, 大槻 勲夫
1967 年 15 巻 12 号 p.
1875-1882
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Pharmacological properties of 2, 3, 4, 5-tetrahydro-1H-2-benzazepine-2-carboxamidine sulfate (GQ-1) has been studied mainly on sympathetic nervous system and the following results were obtained : 1) GQ-1 showed the adrenergic neurone blocking activity three-fifth as potent as that of guanethidine in urethane anesthetized cat nictitating membrane. 2) Unlike with the cases of guanethidine and guanisoquin, GQ-1 did not cause the contraction of the nictitating membrane nor did the rise of the blood pressure in urethane anesthetized cat. 3) GQ-1 potentiated the pressor response to norepinephrine and markedly suppressed the pressor response to tyramine in cat.
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掛見 喜一郎, 有田 隆一, 堀 了平, 小西 良士
1967 年 15 巻 12 号 p.
1883-1887
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Absorption of barbituric aicd derivatives from rat small intestine was investigated systematically, and it was found that the absorption did not depend on chemical structure and lipid solubility so much as in the gastric absorption, but no specialized absorption mechanism was demonstrated. The pH-partition hypothesis was partially operative, but pH absorption profile had an optical pH range in all derivatives investigated and N-methyl series which have higher lipid solubilty than the corresponding oxy series were absorbed slowly than expected. These phenomena of in situ experiments which are assumed exceptional to pH-partition hypothesis were correlated significantly with the in vitro binding to mucosal preparations of rat small intestine.
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井上 重治
1967 年 15 巻 12 号 p.
1888-1895
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Syntheses of the title compounds starting from 2, 6-di-O-p-tolylsulfonyl-tetra-N-acetyl-kanamycin via 6-azido-and 6-hydrazino-2, 3-oxazolinum intermediates. Terminal amination and configurational inversion at C
2 of the 3-amino-glucose moiety were confirmed by nuclear magnetic resonance spectroscopy, molecular rotations and hydrolysis data. The structures of two diamino-derivatives of tetra-N-acetyl-kanamycin obtained as minor products were discussed.
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Yoshiro Kobayashi, Eitatsu Chinen
1967 年 15 巻 12 号 p.
1896-1900
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
All six isomers of bis (trifluoromethyl) pyridine were synthesized by the reaction with corresponding pyridine dicarboxylic acid and SF
4. The characteristic infrared absorption frequencies of this series of compounds were compared with those of similar compounds and the fact that the symmetrical vibration frequencies of aromatic compounds with two trifluoromethyl groups generally shift to the lower side compared with the compounds with a trifluoromethyl group was found.
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小林 義郎, 中野 文雄, 知念 栄達
1967 年 15 巻 12 号 p.
1901-1905
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Fragmentation behavior of trifluoromethylated pyridines was investigated. The results given were as follows : 1) α-cleavage of the substituent is well correlated to the inductive effect of the nitrogen atom of the aromatic ring ; 2) β-cleavage of the substituent is strongly dependent upon the π-electron density on the carbon atom of the ring at the substituted position.
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村田 寿, 和田 忠男
1967 年 15 巻 12 号 p.
1906-1909
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Benhepazone is activated maximally at 395 mμ and emits a fluorescence which shows a maximum at 410 mμ. Furthermore, Benhepazone was found to be quantitatively extracted into chloroform in alkaline conditions from a mixture consisting of Benhepazone and related compounds. On the basis of these findings, a fluorometric method has been adopted for the measurement of Benhepazone in tissues, urine, and feces. A procedure for assaying Benhepazone consists of its extraction with chloroform followed by the measurement of its fluorescence intensity at 410 mμ and it has been ascertained that neither metabolic products of Benbepazone nor native substances in biological samples interfered by the determination of Benhepazone in the course of this procedure.
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亀谷 哲治, 根本 英雄
1967 年 15 巻 12 号 p.
1910-1915
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Chichibabin reaction of 8-methylquinoline (I) in dimethylaniline with sodium amide gave a mixture of 2-amino-8-methylquinoline (II) and 2-amino-3, 4-dihydro-8-methylquinoline (III), the latter of which was characterized as its hydrolyzed product, namely, 3, 4-dihydro-8-methylquinolone (IV). Furthermore, Friedel-Crafts reaction of N-(o-tolyl)-β-chloropropion-amide (V) was examined in order to synthesize an authentic sample (IV) for comparison, but a mixture of 5-methyl-(VI) and 8-methyl-3, 4-dihydrocarbostyril (IV) was obtained unexpectedly. This fact shows the migration of the methyl group was occurred in case of Friedel-Crafts reaction by aluminum chloride without solvent. On the other hand, catalytic hydrogenation of 8-methylcarbostyril (XI) in the presence of 40% palladium-charcoal afforded the above compound (IV), which was also identical with the sample obtained by Chichibabin reaction of I, followed by hydrolysis, and by Friedel-Crafts reaction of V.
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亀谷 哲治, 菅原 宏, 菅野 和子
1967 年 15 巻 12 号 p.
1916-1921
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
One of two compounds, which were obtained by catalytic hydrogenation of VII in dry methanol using one molar equivalent of dry hydrochloride gas in the presence of platinum oxide, was separated after recrystallization from water. The structure of the above compound was characterized to be XV by acetylation and hydrolysis. In the latter case, the carboxylic acid (X) was obtained and found to be identical with an authentic sample, which was obtained by ring contraction of IX.
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矢島 治明, 木野村 保彦, 大島 孝夫, 岡田 芳男
1967 年 15 巻 12 号 p.
1922-1928
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Arginylmethionine was prepared by three different methods, one from N
α-benzyloxycarbonyl-N
G-tosylarginylmethionine with sodium in liquid ammonia and others, from N
α-benzyloxycarbonyl-N
G-nitroarginylmethionine by treatment with hydrogen fluoride, and from N
α-t-butoxycarbonyl-N
G-nitroarginylmethionine by treatment with stannous chloride in 80% formic acid. Arginylmethionine was coupled with N
α-t-butoxycarbonylprolyltyrosine via the azide method and the resulting peptide was treated with trifluoroacetic acid to give prolyltyrosylarginylmethionine, the tetrapeptide situated within the structures of monkey and human β-melanocyte-stimulating hormones.
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ヒキノ ヒロシ, 青田 恵太郎, 竹本 常松
1967 年 15 巻 12 号 p.
1929-1933
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Two sesquiterpenic alcohols, cyperol and isocyperol, have been isolated from nutgrass (Cyperus rotundus (Cyperaceae)) and shown to have stereostructures I and IV, respectively, by means of spectral determinations and by transformations to α-cyperone (II) and 4β (H)-eudesman-3-one (IX), respectively.
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田原 昭, 平尾 健一
1967 年 15 巻 12 号 p.
1934-1938
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
By confluence from l-abietic acid at the key intermediate (XXIV) for Nagata's total synthesis of dl-atisine (I), dl-veatchine (II) and dl-garryine (III), the first example of total synthesis of the natural diterpene alkaloid from the other natural diterpene, was accomplished.
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井深 俊郎, 北野 正彦
1967 年 15 巻 12 号 p.
1939-1943
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
The constitution of homostephanoline was investigated and the complete constitution (I) including the absolute stereostructure was presented.
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井深 俊郎, 北野 正彦
1967 年 15 巻 12 号 p.
1944-1947
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Synthesis of hasubanan derivative from sinomenine is described.
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関 英男, 古賀 憲司, 山田 俊一
1967 年 15 巻 12 号 p.
1948-1954
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
Eleven kinds of ethyl 2-substituted-3-phenylpropionates (Ia∼k) were reduced with sodium borohydride under a similar reaction condition and the effects of the α-substituents on the reduction were examined. Some esters (Ia∼c, e, f, j, k) were hydrolyzed with alkali. The obtained data of hydrolysis rate constants were roughly parallel to those of ester reductions. These results may be explained by considering both inductive and steric effects of the α-substituents.
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奥田 拓男, 吉田 隆志
1967 年 15 巻 12 号 p.
1955-1965
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
The structural correlation of coriamyrtin (I) and tutin (II) was established by deriving both compounds to coriamyrtin-isonorketone-methoxide (XXVIII), as well as to its dihydro derivative (XXX). The absolute configurations of these compounds were determined by the ORD spectra and the benzoate rule. The mutual influences of the 2-hydroxyl group and the terminal epoxide in the NMR spectra were analyzed for tutin and derivatives.
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吉田 圭治, 渡辺 文彦
1967 年 15 巻 12 号 p.
1966-1978
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
17β-Hydroxy-A-nor-5α-androstan-1α, 2α-episulfide (XXIIIa) and -1β, 2β-episulfide (XIa) were prepared from 17β-acetoxy-A-nor-5α-androstan-2-one (Ib) via the corresponding epoxides (XXa) and (IXa) as intermediates.
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星 昭夫, 榑谷 和男
1967 年 15 巻 12 号 p.
1979-1984
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
The absorption of terephthalic acid (TPA) from gastrointestinal tract and its metabolites in urine were studied with radioactive TPA (carboxyl-
14C compound). Terephthalic acid was absorbed mainly from stomach and small intestine and partly from caecum and large intestine. The administered TPA was excreted almost quantitatively in urine within 24 hr. after the administration, and carbon dioxide as the cleavaged product was not found in the expired air. Examinations by thin-layer chromatography and autoradiography technique failed to detect any metabolite in urine. It was concluded that the administered TPA is not metabolized in body and almost all of it is excreted intact in urine.
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神谷 庄造, 越沼 きみえ
1967 年 15 巻 12 号 p.
1985-1988
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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村田 寿, 森 昌弘
1967 年 15 巻 12 号 p.
1988-1990
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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松本 郁男
1967 年 15 巻 12 号 p.
1990-1995
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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富田 真雄, 青柳 良明, 坂谷 芳郎, 冨士谷 憲徳
1967 年 15 巻 12 号 p.
1996-1999
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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川添 豊, 吉岡 佑子, 山田 むつみ, 井下田 浩
1967 年 15 巻 12 号 p.
2000-2002
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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矢内 玲子, 長澤 弘, 榑谷 和男
1967 年 15 巻 12 号 p.
2003-2004
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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福岡 正道, 三橋 博
1967 年 15 巻 12 号 p.
2007-2008
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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伊藤 幸雄, 栗田 宏紀, 山口 東太郎, 佐藤 匡徳, 奥田 朝晴
1967 年 15 巻 12 号 p.
2009-2010
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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清水 文治, 斎藤 彰夫, 西村 卓三, 宮木 美知子
1967 年 15 巻 12 号 p.
2011-2014
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー
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藤野 政彦, 畑中 千年
1967 年 15 巻 12 号 p.
2015-2016
発行日: 1967/12/25
公開日: 2008/03/31
ジャーナル
フリー