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Volume 17, Issue 1
Displaying 1-35 of 35 articles from this issue
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SADAYO SASAGAWA, KAZUKO KANETANI, SHIGEKO KIYOFUJI1969 Volume 17 Issue 1 Pages 1-4
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of xylopinine on the adrenergic mechanism of the isolated guinea-pig's atria were studied. Xylopinine in concentrations above 10-8 depressed the rate of the atrial beat without affecting the concentration. During the early phase of the atrial depression by xylopinine the chronotropic effects of adrenaline and isopropylnoradrenaline were depressed, while the same effects were potentiated during the late phase of the depression.View full abstractDownload PDF (549K) -
SHOICHIRO TAGAMI, KOZABURO SASAYAMA, DENITSU SHIHO1969 Volume 17 Issue 1 Pages 5-10
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA red substance was obtained by the reaction of 2-hydrazino-3-phenylquinoxaline with excess aliphatic aldehyde. The structure of this substance was studied and the reaction rate was found to follow second-order kinetics. From these results, a mechanism was proposed and possible explanations for the red color were discussed.View full abstractDownload PDF (590K) -
HIDEHIKO KANEKO, KEIJI NAKAMURA, YUZURU YAMATO, MIKIO KUROKAWA1969 Volume 17 Issue 1 Pages 11-22
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to examine the relationships between the structure and activity in anabolic steroids, 17α-methyltestosterone and 17α-methyldihydrotestosterone derivatives containing 7α-alkylthio and/or 7α-arylthio groups were synthesized. Some of these compounds possess high myotrophic activity with a favorable myotrophic-androgenic ratio. Preparation of androstano-isoxazoles and isoxazolines having the 7α-ethylthio group was also described.View full abstractDownload PDF (1186K) -
HISASHI NOGAMI, TSUNEJI NAGAI, EIHEI FUKUOKA, TOSHIHISA YOTSUYANAGI1969 Volume 17 Issue 1 Pages 23-31
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution rate constants of barbital polymorphs in water were measured by rotating disk method. The phase transition took place by compression during preparing of the disk. Combining the Levich equation and the concept of consecutive process first proposed by Berthoud, the rate constant of interfacial chemical reaction and that of transport process were obtained separately, and the diffusion coefficient also was calculated. These values were reasonable compared with data found in many references, and the theoretical diffusion coefficient calculated according to the Wilke and Othmer equations. The activation energies of transport process and chemical reactionwere obtained from the temperature dependence. Furthermore, the solubility data obtained by the finite differences diagram method affordedthe heat of transition, transition temperature and entropy change between Phase I and Phase III.View full abstractDownload PDF (845K) -
MINORU SEKIYA, HIDEO SAKAI1969 Volume 17 Issue 1 Pages 32-35
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA variety of N-α-amidobenzyl compounds attached to secondary amines have been newly prepared advantageously by reactions of N, N'-benzylidenebisamines with amides. Also the known procedures for preparation of N, N'-benzylidenebisamines from benzaldehyde was best improved in yield using a dehydrating agent, boron trioxide.View full abstractDownload PDF (490K) -
ATSUSHI KUROSAWA1969 Volume 17 Issue 1 Pages 36-42
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of hydrazine compounds on rabbit liver mitochondrial monoamine oxidase were examined using a manometric method. Two hydrazine derivatives, i.e., 1-benzyl-2-(4, 5, 6, 7-tetrahydro-1, 2-benzisoxazol-3-yl) carbonyl hydrazine hydrochloride (31037-S) and 1-benzyl-2-(3-methylisoxazol-5-yl) carbonyl hydrazine (31087-S) were especially powerful inhibitors of this enzyme. They acted competitively with the enzyme and were more potent than iproniazid. When each inhibitor was allowed to react with the enzyme in the absence of substrate, its inhibitory action was irreversible and much enhanced. Cyanide and oxygen promoted the inhibitory action of both compounds. In comparison with the potencies of some allied compounds, it was suggested that an active part of 31037-S or 31087-S is a benzylhydrazine moiety, and that it directly influences the enzyme active site.View full abstractDownload PDF (826K) -
ATSUSHI KUROSAWA1969 Volume 17 Issue 1 Pages 43-48
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSExaminations were performed to ascertain the prosthetic groups of rabbit liver mitochondrial monoamine oxidase. This enzyme was inhibited competitively by 8-hydroxyquinoline sulfate. Neocuproine and α, α'-dipyridyl were weak inhibitors, but diethyldithiocarbamate or ethylenediaminetetraacetate were little effective. Cupric ions were available to reactivate the depressed activity of the 8-hydroxyquinoline-treated enzyme. Since recovery was not observed with ferrous ions, the enzyme appeared to be cuproprotein. The second prosthetic group was likely to be sulfhydryl because p-chloromercuribenzoate reacted competitively with the enzyme. Oxidants such as 2-methyl-1, 4-naphthoquinone or β-naphthoquinone-4-sulfonate were also strong inhibitors. Inhibitory effects of 1-benzyl-2-(4, 5, 6, 7-tetrahydro-1, 2-benzisoxazo-3-lyl) carbonylhydrazine hydrochloride (31037-S) and 1-benzyl-2-(3-methylisoxazol-5-yl) carbonylhydrazine (31087-S) were counteracted clearly by the simultaneous addition of some metal ions. Cupric ions were especially efficient. An analogous counteraction was observed with cysteine, while methionine was inert in this phenomenon. The inhibitory action of both hydrazine compounds was likely to be dependent on the blocking of these metal and sulfhydryl groups.View full abstractDownload PDF (698K) -
ATSUSHI KUROSAWA1969 Volume 17 Issue 1 Pages 49-53
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdditional effects of 1-benzyl-2-(4, 5, 6, 7-tetrahydro-1, 2-benzisoxazol-3-yl) carbonylhydrazine hydrochloride (31037-S) and 1-benzyl-2-(3-methylisoxazol-5-yl) carbonylhydrazine (31087-S) were demonstrated in the mitochondrial monoamine oxidase of rabbit liver. The potencies of the compounds were greatly enhanced when the enzyme was preincubated for a long time at 37.5° before the addition of substrate and each hydrazine compound. This phenomenon occurred proportionally to time of the preincubation. Although the potenciated effect was observed analogously with both hydrazine compounds, it was much more remarkable in the case of 31087-S, especially when the enzyme was preincubated with semicarbazide. The preincubation did not influence normal enzyme activity. The compounds affected competitively the 3 min-preincubated enzyme, while they showed a non-competitive type inhibition in the 10 min-preincubated one. The phenomena observed here were unlikely based on mechanisms such as the transformation of each inhibitor, damage of the mitochondrial structure or the sensitization of the enzyme by cyanide.View full abstractDownload PDF (640K) -
AKIRA TAHARA, OSAMU HOSHINO, TOMIHIKO OHSAWA1969 Volume 17 Issue 1 Pages 54-63
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPreviously, l-abietic acid (I) was transformed into hydrofluorene derivative, regarded as one of the basic structure of gibberellin, by application of the benzilic acid rearrangement. As successive transformation, a synthesis of c-homohydrofluorene (XX) has been realized by opening of B/C-ring juncture and successive ring closure of Δ8, 9-unsaturated ester (X) prepared from (I).View full abstractDownload PDF (1088K) -
AKIRA TAHARA, OSAMU HOSHINO, TOMIHIKO OHSAWA1969 Volume 17 Issue 1 Pages 64-67
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSc-Homofluorene (VI) having undeniable trans-A/B-ring fusion has been previously synthesized from 1-abietic acid (I). In order to have a standard trans-A/B-ring hydrofluorene (XIII), basic skeleton of gibberellin, c-homofluorene (VI) was chosen as starting material and its seven membered alicyclic C-ring was contracted to benzene ring.View full abstractDownload PDF (565K) -
AKIRA TAHARA, OSAMU HOSHINO, TOMIHIKO OHSAWA1969 Volume 17 Issue 1 Pages 68-74
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHydrofluorene (III) and (IV) prepared by alkaline treatment of cis-dioxo ester (II), was already considered, without reliable evidence, to have cis-A/B-ring fusion. Now, in comparison with standard trans-hydrofluorene (XII) previously reported, the assumption on the structure of IV has been confirmed. Otherwise, stereochemical analysis on catalytic hydrogenation of Δ5, 6-unsaturated hydrofluorene (XIV and XV) is also carried out.View full abstractDownload PDF (873K) -
TADAHIKO OTAKA, SEIICHI OKUI, MITSURU UCHIYAMA1969 Volume 17 Issue 1 Pages 75-81
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of insect-moulting steroid, ecdysterone, on protein synthesis in mouse liver was studied. The administration of ecdysterone caused an early stimulation of protein synthesis, as indicated by the marked increase in the incorporation of 14C-chlorella hydrolysate into hot-acid insoluble protein, as early as 2 hr after the treatment as well as does 4-chlorotestosterone. Ecdysterone was able to exert its stimulatory effect on the protein synthetic ability of microsomes or polysomes, but not S-105 fluid, soluble components for protein synthesis, except in microsomal system. The stimulation induced by ecdysterone was partly insensitive to actinomycin, inhibitor of DNA-dependent RNA synthesis, but the stimulation by 4-chlorotestosterone was completely repressed by it.View full abstractDownload PDF (839K) -
YOSHIHIKO BABA, HIROSHI MIZUSHIMA, HIROSHI WATANABE1969 Volume 17 Issue 1 Pages 82-88
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeveral kinds of heme peptides of cytochrome c were prepared and examined on their two catalytic properties, cytochrome c oxidative effect and peroxidative effect. The unrigid coordination at the sixth ligand place of heme iron in heme peptide was proved to be responsible for the two effects. The characteristic roles of peptide moiety of heme peptide in the effects were also discussed.View full abstractDownload PDF (827K) -
SHIGERU KOBAYASHI, MASARU AZEKAWA, HISASHI MORITA1969 Volume 17 Issue 1 Pages 89-93
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn contrast to results in the literature reported by Hodgson and Jenkinson the Reimer-Tiemann reaction of m-bromophenol yielded four products. Three of these were shown unambiguously to be 2-bromo-4-hydroxybenzaldehyde, 4-, and 6-bromosalicylaldehydes. The other product was assigned to be bromoformylhydroxybenzaldehyde.View full abstractDownload PDF (656K) -
HARUKI NISHIMURA, TOMOKO KINUGASA1969 Volume 17 Issue 1 Pages 94-97
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was found that 2-methylpiperazine-carbon disulfide complex (I) obtained by the reaction of 2-methylpiperazine (II) with carbon disulfide was not 2-methylpiperazine-1-carbodithioic acid, but a mixture composed of 3-methylpiperazine-1-carbodithioic acid (VIII) and 2-methylpiperazine salt of 2-methylpiperazine-1, 4-dicarbodithioic acid (IX), and moreover that there was no possibility of disproportionation between VIII and IX during the treatment.View full abstractDownload PDF (620K) -
YASUO KIKUGAWA, SHIRO IKEGAMI, SHUNICHI YAMADA1969 Volume 17 Issue 1 Pages 98-104
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactions of primary, secondary and tertiary amides with sodium borohydride in refluxing pyridine were examined. Tertiary amides were reduced to the corresponding amines in moderate yield, in case of secondary amide no reaction occured and the starting amide was recovered, primary amides, on the contrary, were dehydrated to nitriles. Especially, when nicotinamide was used, the reduction of pyridine nucleus accompanied by dehydration occured to give 1, 4, 5, 6-tetrahydronicotinonitrile.View full abstractDownload PDF (713K) -
SHOJI OKADA1969 Volume 17 Issue 1 Pages 105-112
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn several aminoquinone derivatives the interaction with nucleic acid and the effects on DNA, RNA, and protein synthesis in Ehrlich mouse ascites tumor cells were investigated in relation to the findings that aminoquinone structures in such antibiotics as actinomycins and mitomycins played an important role on their biological effects as a functional group. The results are as follows : 1. Among the aminoquinone derivatives used for this investigation the compounds of aminoquinone imine or aminophenoxazone type showed to interact with nucleic acid by the method of difference spectrum. Besides, the former interacted with both of DNA (calf thymus DNA) and RNA (yeast tRNA). 2. The type of spectral shifts of aminoquinone imines was found to be different from that of aminophenoxazones, and the interaction of these compounds with nucleic acid was become weak by the addition of Mg2+. 3. All the compounds which interacted with nucleic acid inhibited the synthesis of nucleic acid and protein in Ehrlich mouse ascites tumor cells in vitro, and the order of inhibition in each case was as follows ; DNA>protein>RNA. 4. Among these compounds 2-amino-1, 4-naphthoquinone imine-HCl (ANQI) was remarkable for its intensive inhibition on DNA biosynthesis, that is, the incorporation of thymidine-2-14C into DNA was inhibited almost perfectly at the concentrations of ANQI higher than 5×10-6M, and was depressed as much as 33% even at 5×10-8M. 5. These compounds did not stimulate the degradation of DNA, while that of RNA was somewhat stimulated by ANQI.View full abstractDownload PDF (777K) -
SHOJI OKADA1969 Volume 17 Issue 1 Pages 113-119
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn 2-amino-1, 4-naphthoquinone imine-HCl (ANQI), which had previously been reported to interact with nucleic acid and to inhibit the synthesis of nucleic acid and protein, especially of DNA, in Ehrlich mouse ascites tumor cells in vitro, the details of the interaction with nucleic acid were investigated by the methods of melting experiment for DNA, difference spectrum, equilibrium dialysis, and flow dichroism. The results are as follows : 1. The sites in DNA for attachment of ANQI were the purine base moieties, i.e., both of adenine and guanine. ANQI interacted with a highly polymerized native DNA at the highest degree and hardly interacted with such monomers as bases, nucleosides, and nucleotides. 2. ANQI was found to be able to bind to calf thymus DNA up to the ratio of 2 moles per 4 nucleotides by the method of equilibrium dialysis. This means that ANQI can attach with all the purine bases in DNA. 3. Such bivalent metal ions as Mg2+, Ca2+, Mn2+, Cu2+, Zn2+, and Ba2+ interfered with the interaction between ANQI and DNA. On the other hand, Hg2+ increased the extent of interaction. 4. It was found from the measurement of flow dichroism on DNA-bound ANQI that the orientation of ANQI was nearly parallel with the planes of DNA bases.View full abstractDownload PDF (804K) -
JUNKO MORITA, RYOJI HIROTA, SADATOSHI KIMOTO, TETUO MINESITA1969 Volume 17 Issue 1 Pages 120-123
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIncubation of pentaacetylgitoxin (I) with liver and heart homogenates of rabbits easily caused the fission of acetyl groups in the terminal sugar moiety and gave 3', 3", 16-triacetylgitoxin (IIc) as a main product, respectively, accompanied with small quantities of several partial acetates and gitoxin (IIj). IIc was the intermediate in hydrolysis of I to IIj with dilute alkali.View full abstractDownload PDF (547K) -
TAKAO INOUE, FUJIKO NAKAHATA1969 Volume 17 Issue 1 Pages 124-127
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the leaves of Sambucus chinensis LINDL. were isolated α-amyrin palmitate, ursolic acid and β-sitosterol which was confirmed to contain small amounts of stigmasterol and campesterol by gas-liquid chromatography. α-Amyrin palmitate was the first instance which was obtained as crystals from the natural products. A relatively large amount of potassium nitrate was separated from the water soluble fraction.View full abstractDownload PDF (562K) -
AKIRA TAKAMIZAWA, SAICHI MATSUMOTO, SHOJI SAKAI1969 Volume 17 Issue 1 Pages 128-139
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of thiamine-sodium salt (III) with phenylglyoxal in the presence of carbon dioxide yielded 2-phenyloxalylthiamine (Va) which underwent facile air oxidation to thiamine thiazolone (VI) and phenylglyoxylic acid. Thiamine hydrochloride (I) was also condensed with phenylglyoxal in the presence of triethylamine or sodium hydroxide to give Va. The reaction was applied to a number of α-ketoaldehydes including some heterocyclic glyoxals to give corresponding 2-oxalylthiamine derivatives (Vb-1) which were shown to be convertible into stable acyl derivatives (XIa-r).View full abstractDownload PDF (1407K) -
TOSHIHIKO OKAMOTO, HIROSHI TAKAHASHI, HIROAKI TAKAYAMA, TOMIZO KITAGAW ...1969 Volume 17 Issue 1 Pages 140-144
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn the reaction of 5-, 6-, 7-, and 8-nitroquinoline with potassium cyanide in methanol solution, always two kinds of compound were obtained in a moderate yield. The one was o-methoxyquinoline-carbonitrile, in which the cyano group is introduced in ortho-position to the nitro group and then the nitro group is replaced by a methoxyl group, and the other was 1-aminosoxazoloquinoline, in which the nitro group was reduced to hydroxyamino group and this hydroxyamino group was cyclized to an isoxazole ring with the cyano group introduced at ortho-position of the original nitro group. However, in the reaction of 4-nitroquinoline, 4-methoxyquinoline was obtained as a sole product.View full abstractDownload PDF (604K) -
SEIGORO HAYASHI, MITSURU FURUKAWA, YOKO FUJINO, NAOTO MATSUISHI, TADAS ...1969 Volume 17 Issue 1 Pages 145-149
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to find non-narcotic analgesics, 54 compounds of amino-tert-alcohol, in which a variety of substituent groups were involved at the carbon atom in 1-position and at the amino group, were synthesized by reacting various α-and β-amino acid esters with Grignard reagents. These amino acid esters were readily reacted with alkyl Grignard reagents to give the expected compounds. However, when bulky aromatic Grignard reagents were submitted to react, the reactions were found to stop at the stage of intermediate formation of the corresponding ketones.View full abstractDownload PDF (564K) -
HIROSHI MIURA, TAKAHIDE KIHARA, NOBUSUKE KAWANO1969 Volume 17 Issue 1 Pages 150-154
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the leaves of Podocarpus macrophylla were separated hinokiflavone (III), neocryptomerin (VI), sciadopitysin (VII), podocarpusflavone A, C31H20O10 (VIII), and podocarpusflavone B, C32H22O10 (IX). The latter two of them are new compounds and their structures were deduced by comparison of the chemical shifts of the methyl protons of their acetates. VIII and isoginkgetin (XII) were isolated from the leaves of P. nagi. VII was newly isolated from the leaves of Ginkgo biloba.View full abstractDownload PDF (630K) -
MANKI KOMATSU, TSUYOSHI TOMIMORI, NAOKO MIKURIYA1969 Volume 17 Issue 1 Pages 155-162
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe chemical constituents of Swertia japonica MAKINO were studied. Three kinds of new natural xanthones, named norswertianin (I), swertianin (III) and methylswertianin (V), were isolated from the whole herb of this plant, together with desmethylbellidifolin (X) and bellidifolin (XII). I was identified as 1, 3, 7, 8-tetrahydroxyxanthone. The direct isolation of I from natural source has never been published, although it has derived from decussatin (VII) and/or swertinin (VIII) by demethylation. The structure of III and V were shown to be 1, 7, 8-trihydroxy-3-methoxyxanthone and 1, 8-dihydroxy-3, 7-dimethoxy-xanthone, respectively. At the same time, "swertianol"was revised the structure to 1, 5, 8-trihydroxy-3-methoxyxanthone, which was proved to be identical with bellidifolin.View full abstractDownload PDF (950K) -
SHUICHI HAYASHI, TOSHIKO OKUDE, AKIRA SHIMIZU, TAMON MATSUURA1969 Volume 17 Issue 1 Pages 163-167
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNeutral constituents extracted from Metasequoia glyptostroboides HU et CHENG were investigated and seven steroids, β-sitosterol, stigmasterol, campesterol, stigmast-4-en-3-one, stigmasta-4, 22-dien-3-one, campest-4-en-3-one, and 5α-stigmastan-3, 6-dione, together with α-cadinol, m-cresol, and methyl esters of fourteen fatty acids, were identified. This is the first case that 5α-stigmastan-3, 6-dione, stigmasta-4, 22-dien-3-one, and campest-4-en-3-one were identified from natural products.View full abstractDownload PDF (602K) -
HISASHI NOGAMI, TSUNEJI NAGAI, HIROSHI UCHIDA1969 Volume 17 Issue 1 Pages 168-175
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFollowing the previous discussions on the adsorption of tryptophan based on the hydrophobic bonding mechanism, an examination in detail was carried out in the adsorption of barbituric and thiobarbituric acid derivatives by carbon black from aqueous solution in relation to the size of hydrocarbon chains, making the first step to discuss the correlation between the adsorption and the biopharmaceutical data. Equations were derived to express the relationship between the adsorption and the size of the respective molecule, considering the contributions of hydrophobic and hydrophilic moieties. The results were in good agreement with such equations, indicating that the larger the size of hydrophobic moiety, the more the molecule was adsorbed and that each of two 5-substituted hydrocarbon chains might adopt the parallel orientation to carbon black surface. Calculating the thermodynamic functions of adsorption, it was shown that the larger the size of 5-substituted hydrocarbon chains, the less absolute value of enthalpy change and the greater entropy change were caused by the hydration of molecule accompanying the destruction of iceberg through the adsorption process. A selectivity was not found for the adsorption of such geometrical isomers as pentobarbital and amobarbital by carbon black. Correlating the adsorption with the solubility, the partition coefficient, and the surface tension depressing activity, it was established that carbon black was of hydrophobic surface and that the more hydrophobic the molecule, the easier it was adsorbed.View full abstractDownload PDF (823K) -
HISASHI NOGAMI, TSUNEJI NAGAI, HIROSHI UCHIDA1969 Volume 17 Issue 1 Pages 176-180
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDiscussions on biopharmaceutical phenomena were given on the bases of the adsorption by carbon black from aqueous solution and the permeation through Visking tube of barbituric acid derivatives. The absorption of drug was considered to proceed through the two succesive steps : 1) adsorption or uptake onto the membrane surface and 2) transport through the membrane. The results showed that the absorption might be controlled by adsorption or uptake by membrane. The permeation through Visking tube, as an experimental model for the transport process in the absorption, decreased with the increase of the molecular volume of barbituric acid derivatives, as was explained to be a simple diffusion through pore and was contrary to the actual absorption tendency. Plotting the absorption data6, 11) against the adsorbability of barbituric acid derivatives by carbon black, a very good correlation was given, demonstrating that such an adsorption study was useful to estimate the absorbability in vivo. Plotting the data of the binding to bovine serum albumin13) against the adsorbability of barbituric acid derivatives by carbon black, a good correlation was given, suggesting that the adsorption by such a hydrophobic substance as carbon black might have some relation to the pharmacological action. Moreover, a fairly good correlation was observed between the existing pharmacological data and the adsorbability of barbituric acid derivatives by carbon black.View full abstractDownload PDF (628K) -
MINEO SANEYOSHI, FUMIO SAWADA1969 Volume 17 Issue 1 Pages 181-190
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe following synthetic methods for the preparation of 4-thiouridylic acid homologues from uridine are described. Route A. Mild acid treatment of 2', 3'-O-isopropylidene-5'-O-benzoyl-4-thiouridine (II) followed by phosphorylation by Tener's procedure gave 4-thiouridine 2', (3')-phosphate via 5'-O-benzoyl-4-thiouridine (III). Alkali treatment of II followed by phosphorylation by Tener's procedure gave 4-thiouridine 5'-phosphate via 2', 3'-O-isopropylidene-4-thiouridine (IV). Route B. 2', 3'-Di-O-acetyl-5'-O-trityl-4-thiouridine (V) was prepared by thiation of 2, 3'-di-O-acetyl-5'-O-trityluridine. Alkali treatment of V followed by Tener's phosphorylation gave 2', (3')-phosphate of 4-thiouridine via 5'-O-trityl-4-thiouridine (VI). Mild acid treatment of V followed by Tener's phosphorylation gave 5'-phosphate of 4-thiouridine in satisfactory yield via 2', 3'-di-O-acetyl-4-thiouridine (VII). Route C. Direct phosphorylation of 4-thiouridine with excess amounts of cyanoethylphosphate and dicyclohexylcarbodiimide produced 2', (3')-mono-, 5'-mono-and 2', (3'), 5'-diphosphate of 4-thiouridine. Treatment of the diphosphate with dicyclohexylcarbodiimide gave 4-thiouridine 2', 3'-cyclic, 5'-diphosphate (VIII). 4-Thiouridine 2', 3'-cyclic phosphate (IX) was obtained by treatment of 4-thiouridine 2', (3')-phosphate with same manner or by digestion of VIII with E. coli alkaline phosphomonoesterase. 4-thiouridine 3'-phosphate was prepared by digestion of IX with bovine pancreatic ribonuclease.View full abstractDownload PDF (1183K) -
KEIJI SEKIGUCHI, IKUZO HIMURO, ISAMU HORIKOSHI, TOSHIKO TSUKADA, TAKAK ...1969 Volume 17 Issue 1 Pages 191-199
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe differential thermal analysis (DTA) and the differential scanning calorimetry (DSC) were carried out with various two-component mixtures of organic materials prepared by mechanical mixing, by solidification after fusion and by evaporation of the solution of components. As was expected, when the components did not form a molecular compound, no distinct difference in the thermograms were observed between the kinds of samples except that in the ones for the simple physical mixture, additional small peaks due to polymorphic transition appeared occasionally. On the contrary, the method of sample preparation exerted marked influence on the result, if the molecular compound was formed between components. Usually, the evaporated mixture solidifies in the state of stable equilibrium ; therefore, the DTA and DSC curves were the same as that for the mixture of the isolated compound and one of the components. In the case of the physical mixture which is in the metastable state, the curves showed characteristic peaks of the metastable fusion (endothermic), and of the subsequent compound formation and solidification (exothermic). Thus, by applying DTA or DSC to the physical mixture, a simple method was developed for detecting the molecular compound between organic materials. Also, the heat of formation of the molecular compound could be obtained by reducing the total area of the DSC peaks for the isolated compound from that for the corresponding physical mixture.View full abstractDownload PDF (716K) -
YASUSHI ABIKO, MUNEHIRO TOMIKAWA, YASUHIRO HOSOKAWA, MASAO SHIMIZU1969 Volume 17 Issue 1 Pages 200-201
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (354K) -
YASUHIRO HOSOKAWA, MUNEHIRO TOMIKAWA, OSAMU NAGASE, MASAO SHIMIZU1969 Volume 17 Issue 1 Pages 202-206
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (611K) -
NOBUO ITOH, KYOKO YONEZAWA, KAORU ABE, MASAYUKI ONDA1969 Volume 17 Issue 1 Pages 206-210
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (466K) -
HISAO YAMAGUCHI, TOSHIHIKO OKAMOTO1969 Volume 17 Issue 1 Pages 214-216
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (353K) -
AKIO TSUJI, TOSHIO KINOSHITA, MASANORI HOSHINO1969 Volume 17 Issue 1 Pages 217-218
Published: January 25, 1969
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (308K)
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