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Volume 27, Issue 4
Displaying 1-35 of 35 articles from this issue
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AKIRA KOSASAYAMA, YOSHIFUMI WATANABE, KUNIO HIGASHI, FUMIYOSHI ISHIKAW ...1979 Volume 27 Issue 4 Pages 831-840
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Benzhydryliminoimidazolidine derivatives were prepared by the reactions of benzhydrylamines with 2-methylthio- or 2-chloro-2-imidazoline. The reaction of 1-benzhydryl-2-methylisothiourea or benzhydrylisocyanidedichloride with alkylenediamines gave the many 2-benzhydrylimino-1, 3-diazacycloalkanes (14-21). Compound 14, 15, and 17 were alkylated or acylated to give the ring nitrogen substituted derivatives. The alkyl or acyl derivatives of 2-benzhydryliminoimidazolidine obtained here have two tautomeric form, 2-amino and 2-imino form, which were discussed by use of the NMR spectral data. Some of 2-benzhydrylimino-1, 3-diazacycloalkanes showed hypoglycemic activity.View full abstractDownload PDF (946K) -
AKIRA KOSASAYAMA, TSUNEO KONNO, KUNIO HIGASHI, FUMIYOSHI ISHIKAWA1979 Volume 27 Issue 4 Pages 841-847
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of N-benzhydryl bicyclic guanidines (12) was attempted. The key intermediates, 1-benzhydryl-2-N- or 3-(ω-hydroxyalkyl)-2-imino-1, 3-diazacycloalkanes (4) and (9) were prepared. The intramolecular cyclization of 4 to 12 was not advantageous because of the low yield. On the other hand, the intramolecular cyclization of 9 to 12 resulted in good success. In our synthetic course, imidazo [1, 2-a] [1, 3, 5] oxadiazocine derivative (11), a new ring system, and N1-benzhydryl-N1-[2-(1-pyrrolidinyl) ethyl] urea (13) were isolated as by-products. The N-benzhydryl bicyclic guanidines (12) showed potent hypoglycemic activity.View full abstractDownload PDF (780K) -
AKIRA KOSASAYAMA, TSUNEO KONNO, KUNIO HIGASHI, FUMIYOSHI ISHIKAWA1979 Volume 27 Issue 4 Pages 848-857
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of 2, 2- and 3, 3-diphenylimidazo [1, 2-a] [1, 3] diazacycloalkane derivatives (4) and (5) was attempted. The cyclization of 2-(ω-chloroalkylimino)-4, 4-diphenylimidazolidines (3) was not advantageous because it gave a mixture of 4 and 5 in low yield. 5, 5-Diphenylhydantoin (6) was alkylated at the N3 or O2 position and successive reduction of the remained carbonyl group of the products resulted in success. The 3-N-alkylated compounds (14) prepared from 6 selectively gave 4. The 2-O-ethyl derivative (19) afforded 2-(ω-chloroalkylimino) derivatives (21). Heating 21 gave 2-oxo-bicyclic guanidines (22), and treatment of 21 with sodium hydride yielded 3-oxo-bicyclic guanidines (17) in good yield, respectively. Sodium bis (2-methoxyethoxy) aluminum hydride reduction of 17 and 22, having a carbonyl group in the molecule, gave 4 and 5, respectively. Under the same conditions, N-methyl-2-oxo- or 3-oxo-bicyclic guanidines (18) and (28) gave partially reduced products. The bicyclic guanidines (4) and (5) showed potent hypoglycemic activity.View full abstractDownload PDF (1131K) -
SHIRO YAMAMURA, KUNIYUKI ODA, TOMISHIGE MIZOGUCHI, SEIICHI SAITO, YOSH ...1979 Volume 27 Issue 4 Pages 858-869
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis and adrenergic β-mimetic activities of stereoisomeric 9-aryl-5, 6-dihydroxy-1 H-2, 3, 7, 8, 9, 10-hexahydrobenzo [d, e] quinolines (5), which should be regarded as constrained analogs of the benzylamine (2), the tetrahydronaphthalenes (3) and trimetoquinol (TMQ, 1), are presented. Structure-activity relationships of these compounds were explained in terms of various spatial orientations of the functional groups in these molecules suggested by inspection of Dreiding model. The conformations of 3b-trans and 5b-trans, both of which are potent tracheal relaxants, are the type A orientation of the functional groups where the catechol and trimethoxyphenyl groups are approximately anti to each other. 5b-cis which can not hold the type A orientation was only 1/130 as active as 5b-trans. The spatial orientation of the functional groups in TMQ in the crystalline state was found to be the type A. These results may suggest that the conformation of TMQ required for manifesting its β2-stimulating activity in the biophase is probably similar to that in the crystalline state. Contrary to the previous finding that 2 and 3b-trans were active in both β2 and β1 adrenoceptors, 5b-trans was found to possess high selectivity for β2-adrenoceptors.View full abstractDownload PDF (1308K) -
TERUO TAKAHASHI1979 Volume 27 Issue 4 Pages 870-873
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-Norbornene anhydride-mercury compound (III) was synthesized. Since its infrared spectrum showed the shift of carbonyl absorption to a very low wave number side, O-Hg linkage was considered to be in an ionic form (III'), with the carbon in the bonded to mercury becoming a carbonium ion, suggesting the likelihood of its reaction with nucleophilic reagents. Reactions of III with nucleophilic reagents showed that III is reactive to H2S, KI, and KCN.View full abstractDownload PDF (443K) -
HIROSHI HIKINO, YASUSHI OHIZUMI, CHOHACHI KONNO, KAZUO HASHIMOTO, HARU ...1979 Volume 27 Issue 4 Pages 874-879
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe extracts of two species of Rhododendron leaves and their poisonous principles, grayanotoxin I and III, have been daily administered p.o. to mice and rats for 12 weeks. Behavior, general appearance, mortality, body weight, organ weight, hematology, blood biochemistry, as well as gross and microscopic findings have not revealed any significant effects from the extracts and the toxins in both animals, except for the following changes. Thus, the body weights and the liver weights have generally decreased in the treated mice and in the treated animals, respectively. Decrease of the spleen weights and increase of the serum glutamic-oxalacetic transaminase (GOT) and glutamic-pyruvic transaminase (GPT) levels have been also found in the animals given the extracts and the toxins at a higher dose which, however, has been concluded to be within a normal range of function from pathological examinations. Accumulated data demonstrate that despite of the intense acute toxicity, grayanotoxin I and III exhibit rather weak subchronic toxicity as far as the parameters selected in this study concern, which is possibly due to rapid metabolism and/or excretion.View full abstractDownload PDF (729K) -
AKIRA KOSASAYAMA, KUNIO HIGASHI, FUMIYOSHI ISHIKAWA1979 Volume 27 Issue 4 Pages 880-892
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of linear and angular tricyclic guanidine derivatives, imidazo- or pyrimido-[2, 1-b]- or [1, 2-a] quinazoline derivatives, is described. Cyclization of 2-(ω-chloroalkyl)-4-phenyl-3, 4-dihydroquinazolines (9) gave two isomers and their isolation was troublesome. 2-Aminobenzhydrylaminoalkanols (10) obtained from 2-aminobenzophenone (5) were converted to linear tricyclic guanidine derivatives (3, 12, 13, 14, 15), and other tricyclic compounds (22 and 24) containing an oxygen or a sulfur atom. Reaction of 2-benzoylaminoalkanols (26) obtaired from (5) also gave angular products. Most of the tricyclic guanidine derivatives showed a hypoglycemic activity.View full abstractDownload PDF (1309K) -
TAKASHI NISHIKAWA, MASAYUKI SAITO, HIROAKI KUBO1979 Volume 27 Issue 4 Pages 893-898
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA radioimmunoassay method has been developed for the determination of theophylline in body fluids. The anti-theophylline antibodies were obtained from the rabbits which were immunized with theophylline-bovine serum albumin conjugate. Standard curve for theophylline determination was linear on logit-logarithm graph in the concentration range of 3 to 50μg/(ml of blood plasma). The plasma samples were collected from theophylline-receiving patients, and analyzed by the method. The values correlated well to those determined by the high-performance liquid chromatography (correlation coefficient 0.981, regression line y=0.96x-0.06). This method was accurate, sensitive, simple and suitable for routine assay of large numbers of samples.View full abstractDownload PDF (763K) -
HIROAKI NOMURA, YOSHIO YOSHIOKA, ISAO MINAMI1979 Volume 27 Issue 4 Pages 899-906
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAddition of 5-fluorouracil (1) to the double bond of 2, 3-dihydrofuran (3) without using any catalyst progressed smoothly at an elevated temperature and afforded an equilibrium mixture of 1-(tetrahydro-2-furyl)-5-fluorouracil (5) and 1, 3-bis (tetrahydro-2-furyl)-5-fluorouracil (7). By choosing favourable reaction conditions, each of these compounds was obtained in high yield. Thermal decomposition of 7 gave an equimolar mixture of 3 and 5. At a higher temperature, 5 underwent thermal reaction to yield 1 and 3. Study of the present addition reaction was extended to other 5-substituted uracils (8, R=-H, -CH3, -Cl, -Br, -COOCH3, -CONH2, -CN) which furnished the corresponding 1-(tetrahydro-2-furyl)-and 1, 3-bis (tetrahydro-2-furyl)-derivatives (9-15, 18-23) with high yields. A very small amount of 3-(tetrahydro-2-furyl)-5-substituted uracils (6, 16, 17) by-produced in the reactions was isolated and the structures unequivocally identified.View full abstractDownload PDF (1027K) -
SUMIE YOSHIOKA, HIROYASU OGATA, TOSHIO SHIBAZAKI, AKIRA EJIMA1979 Volume 27 Issue 4 Pages 907-915
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSGlucose accelerated the decomposition of sulpyrine remarkably when it was added to sulpyrine injections. As the reaction products of sulpyrine and glucose, aminopyrine (Am), 4-formylmethylaminoantipyrine (FMAA), and N-[2-(5-hydroxymethyl-2, 3, 4, 5-tetrahydro-2, 3, 4-trihydroxy) furyl] methyl-N-methylantipyrine (MAAG) were isolated. These products were determined separately by means of high performance liquid chromatography in order to study the kinetics and mechanism of the formation of them. Methylamino group in 4-methylaminoantipyrine (MAA), a hydrolyzed product of sulpyrine, reacted reversibly with formyl group in glucose and formed an intermediate (MAA-glu). MAA-glu transformed reversibly to MAAG, which decomposed to Am, as follows ; [numerical formula] The dependence of k3, k4 and k5 on pH suggested that these reactions were catalyzed by specific acid. The reaction pathway of the formation of FMAA were different from that of Am.View full abstractDownload PDF (741K) -
AKIO OHSAWA, TOMIO UEZU, HIROSHI IGETA1979 Volume 27 Issue 4 Pages 916-922
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of pyridazinylmethyllithiums with ketones in tetrahydrofuran afforded hitherto unaccessible tertiary alcohols in satisfactory yields. The alcohols reverted to methylpyridazines and ketones in a basic medium whereas the alcohols yielded the corresponding dehydrated products (i.e., pyridazinylethylenes) on heating in neutral media.View full abstractDownload PDF (691K) -
YASUO FUJIMOTO, TAKESHI SHIMIZU, MASAYUKI OHMORI, TAKASHI TATSUNO1979 Volume 27 Issue 4 Pages 923-933
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new synthetic method for cyclodecanone intermediates (33 and 38) which are useful for the synthesis of not only germacranolide but guaianolide-type sesquiterpenoids is described. Synthesis of dihydrocostunolide, a typical germacranolide, is also described.View full abstractDownload PDF (1179K) -
TAKESHI SHIMIZU, YASUO FUJIMOTO, TAKASHI TATSUNO1979 Volume 27 Issue 4 Pages 934-945
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEpoxidation of germacranolide-type sesquiterpenes (1, 5, 11, 17, 20, and 34) with m-chloroperbenzoic acid in dichloromethane or in a dichloromethane-aqueous sodium hydrogen carbonate biphasic system is described. 5-Hydroxy compounds (11 and 20) gave the corresponding epoxides (7, 21, 22, and 23) with m-chloroperbenzoic acid in a dichloromethane-aqueous sodium hydrogen carbonate biphasic system, while these compounds afforded the cyclized products (12, 29 and 30) with m-chloroperbenzoic acid in dichloromethane.View full abstractDownload PDF (1204K) -
CHIKARA KANEKO, ATSUSHI YAMAMOTO, MARIMI HASHIBA1979 Volume 27 Issue 4 Pages 946-952
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new synthetic method of the 4-substituted indoles from 5-substituted quinoline 1-oxides was developed. The method involves a photochemical ring enlargement of the N-oxides to benz [d]-1, 3-oxazepines and subsequent ring contraction to these indoles under thermal or photochemical conditions. An interesting ring contraction of the 6-alkoxycarbonyl-2-cyanobenz [d]-1, 3-oxazepine to 5-aminoisocoumarins and their ring transformation to the 4-alkoxycarbonylindoles were also disclosed.View full abstractDownload PDF (898K) -
KOJI YAMAKAWA, KIYOSHI NISHITANI, KAORI KASAHARA1979 Volume 27 Issue 4 Pages 953-962
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReduction of α-ketol acetates (5, 6, 7, and 8) of 5α-santanolide with NaBH4 and LiAlH (OBut)3 were investigated. The structure of diol monoacetates (9-16) was determined by means of spectroscopic methods and some chemical transformation reactions, oxidation and acetylation. Their conformations are discussed from their NMR data. O, O-Acyl rearrangement was observed in the NaBH4 reduction of α-ketol acetates (5, 6, and 8). The acid-and base-catalyzed O, O-acyl rearrangements of diol monoacetates (9-16) were also investigated. The acyl migration mechanisms are proposed.View full abstractDownload PDF (1170K) -
YUKIHISA KURONO, HIDEO FUKATSU, TOSHIHISA YOTSUYANAGI, KEN IKEDA1979 Volume 27 Issue 4 Pages 963-968
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo isolate an intermediate, cyclodextrin salicylate, the reactions of phenyl salicylates with cyclodextrin were kinetically investigated in alkaline 22% acetonitrile solution. Even in the alkaline solution, the formation and accumulation of cyclodextrin salicylate was confirmed during the course of the reactions. The possible mechanism was discussed. The deacylation rate of cyclodextrin salicylate was considerably small compared with the uncatalyzed hydrolysis rates of phenyl salicylates and that of the acylation of cyclodextrin.View full abstractDownload PDF (669K) -
AKIRA ITO, YO MORI, SHUN HIRAKAWA1979 Volume 27 Issue 4 Pages 969-973
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAcid and neutral proteinases are distributed in the cervical stroma of the human uterus, and the former activity is about 10 times that of the latter. The acid proteinase was completely separated from the neutral enzyme by Sephadex G-200 gel filtration and the acid enzyme was purified about 630-fold to homogenity by ion-exchange chromato-graphy on DEAE-Sephadex A-50 and rechromatography on Sephadex G-200. The purified acid proteinase showed the optimum pH in the range from 3.4 to 3.6 for acid-and ureadenatured bovine hemoglobins, and was completely inhibited by pepstatin and N-bromosuccinimide. Its molecular weight was calculated to be 4.2×104 by gel filtration on Sephadex G-75. From these results, this enzyme could be identified as cathepsin D.View full abstractDownload PDF (786K) -
HIDEAKI UMEYAMA, SETSUKO NAKAGAWA, TAKASHI FUJII1979 Volume 27 Issue 4 Pages 974-980
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRibonuclease A is well known from X-ray diffraction analysis as an enzyme which changes the conformation, when the substrate binds with the enzyme. Therefore amino acids were rotated in order to simulate the coupling movements of the amino acid side chains, water molecule, and the substrate. From the study of the movements of amino acids and the quantum chemioal calculations, a charge relay structure composed of Asp121, His 119 and a water molecule was simulated in the active site of the ribonuclease A. And the water located in the very position where the hydroxyl group of the water molecule can attack phosphorus of the substrate in the second step of the hydrolysis. Moreover it was reported that Lys 7 as well as Lys 41 may participate in the enzymatic reaction.View full abstractDownload PDF (820K) -
YOSHIO ARATA, KENICHI TANAKA, SHIGEYUKI YOSHIFUJI, SHOICHI KANATOMO1979 Volume 27 Issue 4 Pages 981-983
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHeating of pyrrolizidine N-oxide (V) with an aqueous solution of tartaric acid containing ferric nitrate gave Δ1 (8)-dehydropyrrolizidine (VI), which, on treatment with water in the presence of methyl iodide, gave 1-methyl-perhydroazocin-5-one (IX).View full abstractDownload PDF (470K) -
KIYOSHI HATA, KIMIYE BABA, MITSUGI KOZAWA1979 Volume 27 Issue 4 Pages 984-989
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNonanthraquinonic constituents isolated from the heartwood of Cassia garrettiana CRAIB. (Leguminosae) together with several anthraquinones were shown to be betulic acid, rhamnocitrin, rhamnetin, protocatechuic aldehyde, quercetin, 3, 3'-dihydroxybibenzyl, 3, 3', 4-trihydroxybibenzyl, 3, 3', 4, 5'-tetrahydroxybibenzyl, 3, 3', 4, 5'-tetrahydroxystilbene, and 2, 3, 5, 7-tetrahydroxy-9, 10-dihydrophenanthrene (which was isolated and identified as tetraacetate).View full abstractDownload PDF (868K) -
RYUJI MARUMOTO, YOSHIO YOSHIOKA, TAKEHIKO NAKA, SHUNSUKE SHIMA, OSAMU ...1979 Volume 27 Issue 4 Pages 990-1003
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Mono-and 2, 6-di-substituted cAMP (cAMP : adenosine 3', 5'-cyclic phosphate) were derived from the corresponding adenosine analogs via the 5'-phosphates. 2-Substituted cAMP and aristeromycin 3', 6'-cyclic phosphate were led to the 8-bromo derivatives. 8-(3, 5-Dimethylpyrazol-1-yl)-cAMP was derived from 8-hydrazinoadenosine. 8-(2-Hydroxypropyl-2)-cAMP was prepared by a γ-ray irradiation of cAMP in isopropanol. N6-Butyl-2-phenyl-cAMP was derived from 2-phenylinosine. 2-or 8-Substituted cAMP was led to its dibutyryl derivative. The activities of these new analogs were assessed with cAMP-dependent protein kinases (PK) and cAMP phosphodiesterases (PDE). 8-Bromo-2-chloro-, 2-chloro-, 2-bromo-, 2-phenylthio-, 8-carbamoyl- and 8-carboxy-cAMP were better activators of PK than cAMP, while 2-substituted analogs were significant substrates and inhibitors of PDE. 2-Phenyl-, benzyl-, phenoxy-, chloro- and bromo-cAMP or aristeromycin 3', 6'-cyclic phosphate had an inhibitory effect on the binding of cAMP to PK equal to or more than cAMP.View full abstractDownload PDF (1170K) -
HIROSHI YAMANAKA, HIROSHI EGAWA, TAKAO SAKAMOTO1979 Volume 27 Issue 4 Pages 1004-1008
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of quinoline 1-oxide with 3-aminocrotononitrile or 3-aminocinnamonitrile in the presence of benzoyl chloride afforded 2-methyl-or 2-phenyl-imidazo [1, 2-a] quinoline-1-carbonitriles along with the 2-substituted quinoline derivatives. This reaction was also observed on isoquinoline 2-oxide and 1-methyl- and 1-phenyl-imidazo [2, 1-a] isoquinoline-2-carbonitriles were obtained. The mechanism of the reaction was described tentatively.View full abstractDownload PDF (655K) -
HIROSHI IWASE, YOKO TAKEUCHI, ASAO MURAI1979 Volume 27 Issue 4 Pages 1009-1014
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe fragmentation of twenty kinds of trimethylsilyl derivatives of amines upon electron impact is studied for the possibility of ultramicrodetermination and selective identification of amines by mass fragmentography. In addition, the selective identification of trimethylsilyl derivatives of amino acids and amines in their mass spectra is also examined. The results obtained in this study indicated that the selective identification and ultramicrodetermination of amines by mass fragmentography will be possible by monitoring the intense ion such as m/e 174. The m/e 147 ion is observed for the amines which have O-trimethylsilyl group. Both ions at m/e 147 and 59 are useful for the selective identification of amino acids and amines in their mass spectra. It is not always true that the ion at m/e 147 indicates the presence of O-trimethylsilyl group, considering from the results that this ion is observed for N-trimethylsilyl n-butyl esters and N-trimethylsilyl l-menthyl esters of amino acids.View full abstractDownload PDF (718K) -
HIROSHI ZENDA, KUSUO NARITA, HISAYO KITAMURA, TAKUO KOSUGE1979 Volume 27 Issue 4 Pages 1015-1020
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new method of microdetermination of halogens and sulfur in organic compounds by combustion tube method was examined. It was found that tungsten trioxide among metal oxides was the most appropriate catalyst for oxidation of samples and air as carrier gas was suitable for the analysis. And also, direct introduction of few drops of water into the combustion system was found to be very effective for the analysis. Titration of halogens and sulfur in the combustion product were performed by argentimetric titration at pH 1 with dithizone indicator and by barium perchlorate titration at pH 2 using dinitrosulfonazo-III as indicator, respectively. Whole analysis procedure can be carried out only within 15 minutes.View full abstractDownload PDF (655K) -
HIKARU NAGATOMI, KAZUKO ANDO, MASAHIRO KAWASAKI, BOMPEI YASUI, YASUYOS ...1979 Volume 27 Issue 4 Pages 1021-1029
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of N-diphenylmethyl derivatives of glycine was synthesized and their anti-inflammatory and some other pharmacological properties were studied. The inhibition of carrageenin edema-induction and the protection of albumin from heat denaturation by these derivatives were studied in relation to the substituents in one of the phenyl groups. The most potent compounds, 3, 4-dichloro-(Compd. 22) and 4-fluoro-(Compd. 16) diphenylmethylglycine derivatives, showed the higher activity in carrageenin-edema and weaker toxicity tested by gastric irritation and acute toxicity study than 2-(4-isobutyl-phenyl) propionic acid (ibuprofen). Compd. 16 showed the significant and interesting synergic effect by co-administration with cortisone acetate in the various tests of anti-inflammatory activity.View full abstractDownload PDF (1019K) -
KIKUO ARAKAWA, MITSUTERU HIRATA, KOICHIRO WATANABE, HIROSHI KUGA, EIZO ...1979 Volume 27 Issue 4 Pages 1030-1033
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo analogues of [Ile5]-angiotensin II with the substitution of C-terminal phenyl-alanine by L-α-methyl-3, 4-dihydroxyphenylalanine have been synthesized. The agonistic activity in the rat blood pressure was largely diminished, and the antagonist activity to parent angiotensin II was also much weaker than that of [Sar, 1 Ile8]-angiotensin II. Both two analogues did not act as antagonists to norepinephrine.View full abstractDownload PDF (496K) -
HIDEHARU IKEBUCHI, YASUMASA KIDO, GORO URAKUBO1979 Volume 27 Issue 4 Pages 1034-1038
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSProgressive distribution of 115mCd in the blood and the main 115mCd-binding protein in the red cells were investigated after a single intraperitoneal administration of 115mCd-Cl2 to rabbit. 115mCd in blood decreased drastically on the 1st day after injection and increased sharply again on the 2nd day, then gradually decreased showing the regression equation of Y=-0.019x+3.507. The half life of 115mCd in the blood was calculated to be 158.4 days. On the 14th day after injection of 115mCdCl2 solution, 99.1% of the radioactivity in the whole blood was in the red cells, over 90% of the radioactivity in the red cells existing in the supernatant of stroma-free hemolysate. From the results of gel-filtration, DEAE Sephadex column chromatography and gel-electrophoresis, it was elucidated that about 70% of the radioactivity of the stroma-free hemolysate was bound to thionein. But the ratio of the two components in metallothionein was different between the red cells and the liver. It was also made clear that incorporation of metallothionein into red cells through cell membrane never occurred by incubating red cells with 115mCd-thionein. Considering the observations mentioned above, it was presumed that the metallothionein in the red cells may have originated from some other organ than the liver.View full abstractDownload PDF (613K) -
KANETO UEKAMA, TETSUMI IRIE, FUMITOSHI HIRAYAMA, FUMIO YONEDA1979 Volume 27 Issue 4 Pages 1039-1042
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA laser-irradiation (490 nm) of the tranquilizing phenothiazines such as chlorpromazine, propericiazine, prochlorperazine, and promethazine in the presence of riboflavin gave the corresponding sulfoxides in an acidic buffer solution (pH 4.0). Fluorescence quenching and visible absorption changes of riboflavin by the binding to phenothiazines were quantitatively treated to obtain the equilibrium constants (Kc) of the complexes. The larger the Kc values, the greater the extent of photolysis was observed. Riboflavin-sensitized photooxidation was discussed on the basis of the complex formation between riboflavin and phenothiazines.View full abstractDownload PDF (503K) -
ATSUSHI SUGII, KUMIKO HARADA1979 Volume 27 Issue 4 Pages 1042-1044
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA macroreticular resin containing isothiocyanate group was proposed as an insoluble reagent and applied to the removal of the primary and secondary amines. The reaction condition of this resin with primary and secondary amines were determined. Most of the aliphatic amines tested, except for primary amines having tertiary alkyl group, were retained on the resin by shaking at 50°for 2 hr. Three kinds of impurities in commercial triethylamine could be removed by using this resin.View full abstractDownload PDF (448K) -
MOTOICHI MIYAZAKI, YASUHISA TAGUCHI1979 Volume 27 Issue 4 Pages 1045-1048
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe behavior of copper and nickel chelates of β-ketoimines and the related 3-bromo-β-diketone were investigated by electron capturing detector-gas chromatography (ECD-GC). The chelate, bis (4-imino-2-pentanono)-nickel (II) gave the most sharp gas chromatogram among the chelates examined. The β-ketoimine chelates showed to be less sensitive towards ECD-GC than the chelates of the original β-diketone and the related 3-bromo-β-diketone. Approximate values of detection limits for metals were also obtained by ECD-GC on some of the copper and nickel chelates here examined.View full abstractDownload PDF (479K) -
SOLMAZ DOGANCA, AYHAN ULUBELEN, TSUTOMU ISHIKAWA, HISASHI ISHII1979 Volume 27 Issue 4 Pages 1049-1050
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(+)-Peucedanol methyl ether was isolated from Hippomarathrum cristatum (Turkish Umbelliferous plant), and the circular dichroism curves of it in MeOH and CHCl3 were determined.View full abstractDownload PDF (360K) -
MINORU KUBOTA, TADAMASA HIRAYAMA, OSAMU NAGASE, HARUAKI YAJIMA1979 Volume 27 Issue 4 Pages 1050-1054
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethanesulfonic acid was employed as a deprotecting reagent for the syntheses of the hexadecapeptide and the heptadecapeptide corresponding to α-endorphin and γ-endorphin. Their analgesic potencies were 0.021 and 0.013 relative to that of morphin respectively.View full abstractDownload PDF (722K) -
SHIGERU OHMIYA, KIMIO HIGASHIYAMA, HIROTAKA OTOMASU, JOJU HAGINIWA, IS ...1979 Volume 27 Issue 4 Pages 1055-1057
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new type of lupin alkaloid, tsukushinamine (I) was isolated together with six known alkaloid, (-)-cytisine, (-)-rhombifoline, (-)-N-formylcytisine, (-)-anagyrine, (-)-baptifoline and (±)-ammodendrine, from the epigeal parts of Sophora franchetiana Dunn (Leguminosae). The structure of I was presumed to be a new type of tetracyclic lupin alkaloid by spectral data.View full abstractDownload PDF (445K) -
YUICHI HASHIMOTO, KOICHI SHUDO, TOSHIHIKO OKAMOTO1979 Volume 27 Issue 4 Pages 1058-1060
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA mutagen, 3-amino-1-methyl-5H-pyrido [4, 3-b] indole (Trp-P-2, 1), was reacted with DNA in the presence of rat liver microsomes. One of the modified bases was identified as 3-(C8-guanyl) amino-1-methyl-5H-pyrido [4, 3-b] indole (2).View full abstractDownload PDF (448K) -
HARUAKI YAJIMA, SUSUMU FUNAKOSHI, NOBUTAKA FUJII, KENICHI AKAJI, HIROS ...1979 Volume 27 Issue 4 Pages 1060-1061
Published: April 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of S-p-methoxybenzylcysteine sulfoxide with hydrogen fluoride or methanesulfonic acid in the presence of anisole afforded S-p-methoxyphenylcysteine as a major product, while S-benzylcysteine sulfoxide resisted to the action of these deprotecting reagents in peptide synthesis. Thiophenol was found to be a powerful reducing reagent of the sulfoxides.View full abstractDownload PDF (352K)
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