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Volume 28, Issue 12
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YOSHIHISA KURASAWA, ATSUSHI TAKADA1980 Volume 28 Issue 12 Pages 3457-3465
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of N-(1, 2-bisethoxycarbonylvinyl)-o-aminoacetophenone (IVc) with an excess of hydrazines or guanidines gave 4-hydroxy-1-oxo-1, 2-dihydropyridazino [4, 5-b]-quinolines (Ia, b) or 1, 3-dioxo-1, 3-dihydropyrrolo [3, 4-b] quinolines (IIIc, d), respectively. It was found that 2, 3-bishydrazinocarbonyl-4-methylquinolines (VIa, b) were converted to 4-hydroxy-1-oxo-1, 2-dihydropyridazino [4, 5-b] quinolines (Ia, b) and 1, 3-dioxo-1, 3-dihydropyrrolo [3, 4-b] quinolines (IIIa, b) under different reaction conditions.View full abstractDownload PDF (886K) -
HIDEO SAWADA, SHINGO ASANO, HITOMI MARUYAMA, MICHIO SHINODA, YASUNORI ...1980 Volume 28 Issue 12 Pages 3466-3472
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe activity of partially purified erythrocyte acid phosphatase (EAPase) was enhanced by alcohols, 7.6-fold by methanol, 4-fold by butanol, 3-fold by propanol, and 2.6-fold by ethanol and by pentanol. The carbon number of the aliphatic alcohols was proportional to the activation rate (defined as half the most activated value per the alcohol concentration) of EAPase, except in the case of ethanol. This rule was also applicable to human prostatic acid phosphatase (PAPase). However, the extent of PAPase activation by alcohols was lower than that of EAPase. In the presence of polyhydric alcohols, sorbitol, glycerin, and ethylene glycol, the extent of activation of EAPase was found to be proportional to the number of hydroxyl groups of the alcohols. The activation of EAPase was analyzed by means of the Lineweaver-Burk plot, and was found to be noncompetitive. PAPase activation by aliphatic alcohols was also noncompetitive.View full abstractDownload PDF (775K) -
TAKAO KONOSHIMA, HIDEO INUI, KEIKO SATO, MARI YONEZAWA, TOKUNOSUKE SAW ...1980 Volume 28 Issue 12 Pages 3473-3478
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree triterpenoid saponins were isolated from legumes of Gleditsia japonica cv.'Saponifera'(Leguminosae). These saponins are rare examples of triterpenoid saponins containing monoterpenes. The desmonoterpenyl compound, C74H120O38, [α]23D -42.3°(MeOH), which was obtained from them by alkali hydrolysis with K2CO3, was characterized as a 3, 28-O-bisglycoside on the basis of physical data and degradation products.View full abstractDownload PDF (725K) -
YUKIHO KUBOTA, TAKAYUKI FUNAKOSHI, SHOZO SHOJI, MINEHIRO MORIYAMA, HIR ...1980 Volume 28 Issue 12 Pages 3479-3487
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCarboxypeptidases CUa and CUb were both shown to be glycoproteins by amino acid and carbohydrate analyses. The numbers of amino acid, hexose, and hexosamine residues were 811, 26 (as galactose), and 6 (as glucosamine), respectively, for carboxypeptidase CUa and 868, 42, and 8, respectively, for carboxypeptidase CUb. Both enzymes were almost completely inhibited by sodium dodecylsulfate and cetyltrimethyl ammonium bromide, but not by Brij-35, Tween 80, or Triton X-100. The enzymes were also inactivated by glycine ethyl ester in the presence of 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide, p-bromophenacyl bromide, phenylglyoxal, AgNO3, CH3HgCl, urea, and guanidine. When the enzymes were incubated with 203Hg-labeled p-chloromercuribenzoic acid ([203Hg] PCMB), approximately 0.2 mol of [203Hg] PCMB was incorporated into them at pH 5.5 with no change in the enzymatic activity. After the denaturation of the enzymes with urea and guanidine, the incorporation of [203Hg] PCMB increased to 2-3 mol per mol of enzyme. The values of Km, Vmax, and kp for the hydrolysis of Z-Glu-Phe were 7.7×10-2M, 222 μmol/l·min·mg, and 2.4×104 min-1, respectively, for carboxypeptidase CUa and 7.1×10-2M, 125 μmol/l·min·mg, and 1.6×104 min-1, respectively, for carboxypeptidase CUb. Diisopropylfluorophosphate, phenylmethanesulfonyl fluoride and HgCl2 inactivated the enzymes with decreases in the values of Vmax and kp but with no change in that of Km, indicating that they are noncompetitive inhibitors of both enzymes. 3-Phenylpropionic acid, which inhibited the enzymes reversibly, increased the value of Km without changing those of Vmax and kp and thus is a competitive inhibitor.View full abstractDownload PDF (982K) -
AKIO OHSAWA, YOSHIHITO ABE, HIROSHI IGETA1980 Volume 28 Issue 12 Pages 3488-3493
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSVarious 3-alkynylpyridazines have been prepared by cross-coupling of 3-halopyridazines and monosubstituted acetylenes in Et2NH with Pd (PPh3)2Cl2-CuI as a catalyst. Though the alkynylation of 3-chloropyridazine 1-oxides afforded 3-alkynylpyridazine 1-oxides, attempts to obtain 3-chloropyridazine 2-oxides were unsuccessful. N-Oxidation of 3-alkynylpyridazines with m-chloroperbenzoic acid yielded their 1-oxides exclusivelyView full abstractDownload PDF (638K) -
SADAO OIDA, AKIRA YOSHIDA, EIJI OHKI1980 Volume 28 Issue 12 Pages 3494-3500
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDisplacement reactions of the acetoxy group in 4-acetoxy-2-azetidinone (2) with aluminum enolates afforded 4-alkylazetidinones 4a, 5a, 10 and 11. The conversion of these azetidinones into 1-carba-penem or -penam compounds was studied.View full abstractDownload PDF (931K) -
TOSHIO KINOSHITA, YAYOI HIRAGA1980 Volume 28 Issue 12 Pages 3501-3506
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA sensitive method for the fluorophotometric assay of creatinine and creatine was established by using a novel enzyme system, creatinineamidohydrolase-creatineamidinohydrolase-sarcosine oxidase-peroxidase system. Diacetyldichlorofluorescin, which has been regarded as a stable storage form of dichlorofluorescin, was found to react readily with peroxide in the presence of peroxidase in a buffer, (pH 7.7) to give intense fluorescence. This reagent was employed for the estimation of hydrogen peroxide generated by the action of the above enzyme system on creatinine and creatine. The present method is highly sensitive and only 20 μl of serum is required for each assay. Ascorbic acid, bilirubin and uric acid, which often affect enzymatic assay methods that utilize peroxidase, did not interfere with the present method. Excellent recovery from human serum was observed for both creatinine and creatine. The results obtained by the present method showed a good correlation with those obtained by the Jaffe method.View full abstractDownload PDF (598K) -
TSUNEJI UMEDA, HIROKO IMANISHI, EIZO HIRAI1980 Volume 28 Issue 12 Pages 3507-3513
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel fluorimetric method is described for the determination of 5-phenyl-3-isoxazolecarboxylic acid (PIA) by using 2-hydroxy-1-naphthalenecarbaldehyde (HNA) ; this method was utilized to provide a specific and sensitive assay procedure for perisoxal in plasma. The developed fluorophore was 3-benzoyl-5, 6-benzocoumarin (BBC), obtained by Knoevenagel condensation of benzoylacetonitrile with HNA, followed by cyclization. Linear relationships between fluorescence intensity and concentration existed over the concentration range of 35-350 ng/ml of PIA and 70-700 ng/ml of perisoxal in plasma. This method is 70 times more sensitive than the colorimetric method reported previously.View full abstractDownload PDF (735K) -
FUMIO YONEDA, KENYA MORI, MASAMI ONO, YOKO KADOKAWA, ETSUKO NAGAO, HIR ...1980 Volume 28 Issue 12 Pages 3514-3520
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of 6-(N-alkylanilino)-2-phenylpyrimidin-4 (3H)-ones, which were prepared by the condensation of 6-chloro-2-phenylpyrimidin-4 (3H)-one with N-alkylanilines, with the Vilsmeier reagent (dimethylformamide-phosphoryl chloride) gave the corresponding 10-alkyl-2-deoxo-2-phenyl-5-deazaflavins (III) in excellent yields. Heating of 6-chloro-5-formyl-3-phenyluracil with N-alkylanilines in dimethylformamide gave the corresponding 10-alkyl-3-phenyl-5-deazaflavins (VI) in a single step. The abilities of the 5-deazaflavins (III) and (VI) thus obtained to oxidize benzyl alcohol and benzylamine were compared, and some automatic recycling of the oxidation reactions was observed. The reaction of compounds III with benzylamine exceptionally gave the adducts, 5-benzylamino-2-deoxo-2-phenyl-5-deazaflavins.View full abstractDownload PDF (646K) -
EIKO HIRANO, KAZUHIRO MORIMOTO, TOSHIYUKI TAKEEDA, YASUO NAKAMOTO, KAT ...1980 Volume 28 Issue 12 Pages 3521-3526
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIbuprofen (IP) gel preparations made by suspending IP in a polyacrylic acid aqueous gel were administered rectally to rats by an in situ rectal loop method, and the IP plasma levels were determined. In addition, the IP release rate from gel preparations was examined in vitro and the correlation with the in situ data was investigated. In the case of IP gel preparations with a higher viscosity or a lower pH, IP plasma levels were maintained for a longer period and the IP release rate from the gel preparation was small. IP plasma levels reached their peaks between one and two hours. The AUC by rectal administration was not influenced by the viscosity or pH of the gel preparation and was about twice the AUC by oral administration. Thus, it appears that aqueous polyacrylic acid gels are useful as a base for rectal drug administration ; the duration of high IP plasma level can be controlled by changing the viscosity and pH.View full abstractDownload PDF (660K) -
MIKIO MASADA, YOSHIHIRO KURODA, TERUMICHI NAKAGAWA, TOYOZO UNO1980 Volume 28 Issue 12 Pages 3527-3536
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNew metabolites have been found in human urine after the oral administration of some amino-penicillins. HPLC analysis showed that the amino-penilicillin metabolite had the same retention time as an in vitro degradation product of the corresponding penicilloic acid in dilute HgCl2 solution or in NaH2PO4 solution. The product was not formed by the same treatment of the intact penicillin. NMR, Raman, and FD mass spectra of the product and the visible absorption spectrum of its colored derivative indicated cleavage of the C-S bond in the thiazolidine ring of the penicilloic acid to leave an SH group. These findings indicate that the metabolite is the penamaldic acid of the parent penicillin. Direct evidence for the presence of the penamaldic acid was obtained from the 200 MHz 1H NMR spectrum of a urine specimen taken after drug administration. Ampicillin and amoxycillin gave metabolites of this kind, but cyclacillin gave no detectable amount of the corresponding metabolite.View full abstractDownload PDF (973K) -
YOSHIHISA KURASAWA, ATSUSHI TAKADA1980 Volume 28 Issue 12 Pages 3537-3541
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Substituted 1, 2-dihydropyridazino [3, 4-b] quinoxalines (VII, VIIIa, and VIIIb) were synthesized from 3-(N, N-dimethylaminocarbonyl) furo [2, 3-b] quinoxaline hydrochloride (I) via 3-oxo-2-(2'H-pyrido [1', 2'-a] pyrimidin-2'-on-3'-yl)-3, 4-dihydroquinoxaline (III) and 3-chloro-2-(2'H-pyrido [1', 2'-a] pyrimidin-2'-on-3'-yl) quinoxaline (V).View full abstractDownload PDF (548K) -
TAKASHI ABIKO, IKUKO ONODERA, HIROSHI SEKINO1980 Volume 28 Issue 12 Pages 3542-3548
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe octacosapeptide corresponding to the entire amino acid sequence of thymosin α1 was synthesized using the catalytic hydrogenation procedure at the final deprotection step. The depressed E-rosette forming capacity of lymphocytes caused by a serum factor from a patient in the active stage of MCNS was significantly restored when the lymphocytes were incubated with thymosin α1. The relative potency of the decapeptide fragment (positions 19-28) was 1.04 and that of the pentadecapeptide fragment (positions 14-28) was 9.83 based on synthetic thymosin α1 (100.00) as a standard.View full abstractDownload PDF (845K) -
YASUO ODA, HIROKO TAGUCHI, NOBUTAKA MASAOKA, KAZUO MINAMI, SUSUMU HOND ...1980 Volume 28 Issue 12 Pages 3549-3554
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTheanine, an antimetabolite of L-glutamic acid, is a weak antibacterial agent. In the hope of obtaining theanine derivatives which have more potent biological activities, a series of theanyl-L-alanine oligopeptides, H-Tea-L-Alan-OH (n=1, 2, 3), and several derivatives of these peptides with blocking groups at the amono-and/or carboxyl-termini were prepared, and their antibacterial and anti-glutamic decarboxylase activities were examined. Theanyl-L-alanine and theanyl-L-alanyl-L-alanine inhibited the growth of Staphylococcus aureus and Escherichia coli most strongly, the percent inhibitions being 2 to 23 times higher against S. aureus or 3 to 4 times higher against E. coli than those of theanine. Structural modifications at the end groups of the peptides, especially N-acylation, caused marked reductions in the antibacterial activities. None of the theanine and theanyl-L-alanine oligopeptides possessed any significant ability to inhibit bacterial glutamic decarboxylase even at a concentration of 50 μmol/ml.View full abstractDownload PDF (644K) -
HARUHISA KIZU, TSUYOSHI TOMIMORI1980 Volume 28 Issue 12 Pages 3555-3560
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour triterpenoid prosapogenins named CP2b, CP3b, CP9 and CP10 were isolated from the alkaline hydrolysate of the crude saponin obtained from the root of Clematis chinensis OSBECK. On the basis of chemical and physicochemical evidence, they were characterized as follows : CP2b (I), oleanolic acid 3-O-β-D-xylopyranosyl-(1→2)-α-L-arabinopyranoside ; CP3b (IV), hederagenin 3-O-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside ; CP9 (V), oleanolic acid 3-O-β-D-glucopyranosyl-(1→4)-β-D-glucopyranosyl-(1→4)-β-D-ribopyranosyl-(1→3)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside ; CP10 (X), hederagenin 3-O-β-D-glucopyranosyl-(1→4)-β-D-glucopyranosyl-(1→4)-β-D-ribopyranosyl-(1→3)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside.View full abstractDownload PDF (812K) -
MASAYUKI KUZUYA, TAMOTSU USUI, SEIJI ITO, FUMIO MIYAKE, SHIGENORI NOZA ...1980 Volume 28 Issue 12 Pages 3561-3569
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHeating of crystal violet lactone (CVL) (1a) and its analogs with hydrazine hydrate afforded a single product in each case, to which the 4, 4-diaryl-3, 4-dihydro-1 (2H)-phthalazinone structure (2) was assigned. Kinetic data showed that the introduction of a dimethylamino substituent in 3, 3-diarylphthalides (1) led to an increase in the rate of formation of the dihydrophthalazinone (2). Thus, the reaction seems to occur by a mechanism which involves a carbonium intermediate. Replacement of 3, 3-diaryl groups on the phthalide by a xanthyl group resulted in the formation of an N-aminophthalimidine derivative on similar treatment. The dihydrophthalazinone (2a) exhibited a greenish-blue color on exposure to a weak acid, indicative of heterolytic ring cleavage to form the dye cation, whereas treatment of 2a with a strong acid resulted in a facile conversion to the N-aminophthalimidine (6) and CVL (1a) in a ratio of ca. 2 : 1.View full abstractDownload PDF (961K) -
AKIO OHSAWA, HEIHACHIRO ARAI, HIROSHI IGETA1980 Volume 28 Issue 12 Pages 3570-3575
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermal decomposition of 2H-[1, 2, 4] oxadiazolo [2, 3-a] pyridine-2-thione afforded 3-(2-pyridyl)-2H-pyrido [1, 2-a]-1, 3, 5-triazine-2, 4 (3H)-dione and 1, 3-di (2-pyridyl) urea, and similar decomposition of its pyridazine analog afforded 3-(3-pyridazinyl)-2H-pyridazino [1, 6-a]-1, 3, 5-triazine-2, 4 (3H)-dione and 1, 3-di (3-pyridazinyl) urea. Aza-heteroaromatic α-isocyanates, which are intermediates in the decomposition, were utilized for the synthesis of unsymmetrical 1, 3-disubstituted ureas.View full abstractDownload PDF (729K) -
FUMIO YONEDA, KAZUO SHINOZUKA, KEIKO HIROMATSU, RYOKO MATSUSHITA, YOSH ...1980 Volume 28 Issue 12 Pages 3576-3583
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of 5-nitro-6-(N-substituted-anilino) uracils (I) with the Vilsmeier reagent (dimethylformamide-phosphorus oxychloride) gave the corresponding 8-chloroisoalloxazines (8-chloroflavins) (II) in a single step. The conversion of I into II probably proceeds via the intermediate formation of the corresponding isoalloxazine 5-oxides (flavin 5-oxides). In fact, treatment of flavin 5-oxides with the Vilsmeier reagent also gave the 8-chloroflavins. Under the same conditions, 7-bromoflavin 5-oxides did not give the corresponding 7-bromo-8-chloroflavins, but the deoxygenated 7-bromoflavins were obtained. In this case, the Vilsmeier reagent acted as a reducing agent as well as a dehydrating and chlorinating agent. The 8-chloroflavins were converted into 8-(substituted-amino) flavins by treatment with appropriate amines.View full abstractDownload PDF (698K) -
KEIJI SEKIGUCHI, MOTOKO KANKE, YASUYUKI TSUDA, KENICHI SHIROTANI1980 Volume 28 Issue 12 Pages 3584-3594
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdduct formation with NH3 was confirmed with 6 sulfonamides (sulfadimethoxine, sulfamethoxazole, sulfanilamide, sulfaphenazole, sulfisomidine, and sulfisoxazole). The thermal and physico-chemical properties of these adducts were investigated by differential scanning calorimetry, thermogravimetry, X-ray powder diffractometry, infrared spectroscopy, and scanning electron microscopy. It was found that one, two or even three kinds of NH3 adducts were formed by the above sulfonamides. When the specific surface areas of the sulfonamides recovered by desorbing NH3 from the adducts were measured by a gas adsorption (BET) method, their particle sizes were found to have been effectively reduced. In addition, variations often found in the DSC and TG curves of these adducts are discussed.View full abstractDownload PDF (1318K) -
MASAYOSHI YAMAGUCHI, MASATSUGU KURA, SHOJI OKADA1980 Volume 28 Issue 12 Pages 3595-3600
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSZinc metabolism in rat liver was investigated after a single oral administration of zinc sulfate. After the administration of 20 mg Zn per 100 g body weight, the zinc accumulated in the liver and pancreas, but not significantly in the kidneys, heart, spleen or lungs. The amount of zinc excreted into the bile was much less than that accumulated in the liver. On the other hand, the elevation of zinc content in the serum caused a significant increase of zinc in the plasma membrane and the cytosol fractions of the liver cells. However, additional increase of zinc in the serum did not further enhance the elevation of zinc content in the plasma membrane and the cytosol fractions. Upon gel filtration on Sephadex G-75 of the serum and cytosol obtained after zinc administration, the accumulated zinc in the serum was mainly eluted at the void volume, while the metal in the cytosol was largely eluted at 1.8 times the void volume, suggesting that the protein-bound zinc in the serum is not directly transported into the liver cells. The present study suggests that the liver is a target organ of zinc in rats and that zinc taken up by the liver cells is stored by binding of the metal to cytosolic proteins.View full abstractDownload PDF (669K) -
SATOSHI HORII, HIROSHI FUKASE, EIJI MIZUTA, KAZUNORI HATANO, KOMEI MIZ ...1980 Volume 28 Issue 12 Pages 3601-3611
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSChemical degradation and spectral studies on toromycin, an antibiotic isolated from Streptomyces collinus subsp. albescens, showed that toromycin is a polycyclic aromatic hydrocarbon having a C-glycosyl group at C-4, a vinyl group at C-8, two methoxyl groups at C-10 and C-12, and a phenolic hydroxyl group at C-1 of 6-oxo-6H-benzo [d] naphtho-[1, 2-b] pyran (1).View full abstractDownload PDF (1261K) -
CHIAKI MORIWAKI, HIROYUKI FUJIMORI, YASUYUKI TOYONO, TOSHIHIKO NAGAI1980 Volume 28 Issue 12 Pages 3612-3620
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSKallikrein [EC 3.4.21.8] was extracted from rat small intestine and purified by acetone fractionation, DEAE-Sephadex A-50 chromatography, Sephadex G-100 gel filtration, hydroxylapatite chromatography, Sephadex G-50 gel filtration and Ampholine isoelectric focusing. Rat intestinal kallikrein (RIK) was separated into 4 or 5 active components and the isoelectric points of the two main fractions were 4.18 (RIK-A) and 4.03 (RIK-B). The final preparations of RIK-A and -B were homogeneous in disc electrophoresis in polyacrylamide gel and their vasodilator activities were 160 and 90 KU per A280, respectively. The molecular weights of RIK-A and -B were estimated by Sephadex G-100 gel filtration to be 33000 and 35000, respectively, while the values obtained by SDS-polyacrylamide gel electrophoresis were both 32000. The amino acid compositions of the two RIK's were similar. The Km values of RIK-A against BAEE and TAME were 0.11 and 0.09 mM, and those of RIK-B were 0.08 and 0.11 mM, respectively. For both RIK-A and -B the optimal pH for hydrolysis of BAEE was 9.2, and both enzymes were stable at pH 7-9. The substrate specificities of RIK-A and -B were similar to that of rat pancreatic kallikrein. Both RIK's were inhibited by aprotinin and leupeptin, but not by SBTI, LBTI, antipain, pepstatin, or chymostatin.View full abstractDownload PDF (975K) -
SEIICHI UESUGI, TOSHIO SHIDA, MORIO IKEHARA1980 Volume 28 Issue 12 Pages 3621-3631
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree dinucleoside monophosphates containing 8, 2'-anhydro-8-thio-9-β-D-arabinofuranosyladenine (As) and its hypoxanthine derivative (Is), AspIs, IspAs and IspIs, were synthesized. Examination of their properties by ultraviolet absorption, circular dichroism and 1H nuclear magnetic resonance measurements and comparison with the properties of AspAs, which has been shown to take a left-handed stacked conformation, showed that all these dimers take a left-handed stacked conformation, and the order of extent of stacking is AspAs≈IspAs>AspIs≈IspIs. This sequence dependency of stability of stacking can be explained in terms of the mode of base-base overlap in a left-handed stack. A similar explanation may be applicable to the corresponding sequence dependency of natural dimers with a right-handed stack.View full abstractDownload PDF (1208K) -
HIROKI TAKAHATA, HIDEO OKAJIMA, TAKAO YAMAZAKI1980 Volume 28 Issue 12 Pages 3632-3638
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSyntheses of 5, 9- and 8, 13-diazasteroids (15) and (19) employing reductive annulation with LiAlH4 are described. The stereochemistry of 15 and 19 is discussed.View full abstractDownload PDF (788K) -
MINEO FUKUI, YUMIKO ENDO, TAKESHI OISHI1980 Volume 28 Issue 12 Pages 3639-3648
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNucleophilic aromatic substitution reactions of chlorobenzenes with the methoxide anion were found to proceed smoothly even in cases where electron-donating groups were present in the same aromatic ring when the chlorobenzenes were activated by chromium tricarbonyl complex formation and when the effectiveness of the methoxide anion was enhanced by the use of 18-crown-6. Application of the present method to indoline or tetrahydroquinoline systems was then examined and 5-chloro-1, 3, 3-trimethylindoline was successfully converted to the corresponding 5-methoxy or 5-benzyloxy compound.View full abstractDownload PDF (1189K) -
MIKIO YAMAZAKI, EMI OKUYAMA1980 Volume 28 Issue 12 Pages 3649-3655
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new oxaphenalenone dimers, bacillosporins A-C, and one known xanthone carboxylic acid, pinselin, were isolated from a fungus, Talaromyces bacillosporus. Bacillosporin A (1) is an acetyl derivative of B (2). Bacillosporin A was transformed to xenoclauxin (5), a known oxaphenalenone dimer, by 2, 3-dichloro-5, 6-dicyanobenzoquinone (DDQ) oxidation. The hemiketal structure of bacillosporin C (7) was proposed on the basis of the spectral data for the compound itself and the hydrogenolysis product (9).View full abstractDownload PDF (830K) -
MICHIO MOTOHASHI, YOSHIKAZU WADA, KAMIYA KAZUHIDE, MASAO NISHIKAWA1980 Volume 28 Issue 12 Pages 3656-3661
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe crystal structure of (±)-trans-2-cyclobutylamino-5, 6-dihydroxy-1, 2, 3, 4-tetrahydro-1-naphthalenol hydrobromide, a potent β-adrenergic stimulant, has been determined by X-ray diffraction techniques. The compound crystallizes from water in the triclinic space group P1 with a=9.198 (1), b=10.472 (2), c=8.020 (1) Å, α=109.09 (2), β=78.20 (1), γ=102.55 (2)°. The structure was solved by the heavy atom method, and the final R for 1300 independent reflections measured with a four circle diffractometer was 5.0%. The cyclohexene moiety of the compound is in a half-chair conformation, with both the benzylic hydroxyl and the substituted amino groups occupying diequatorial positions. Comparison of the crystal structure with that of dl-isoproterenol sulfate shows that both compounds have similar conformations of the aliphatic side chain moiety, including the alkyl amino side chain.View full abstractDownload PDF (620K) -
KAORU FUJI, TAKEO KAWABATA, EIICHI FUJITA1980 Volume 28 Issue 12 Pages 3662-3664
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new combination system consisting of boron trifluoride etherate and dimethyl sulfide has proved to be useful especially for the selective removal of the benzyl protecting group in a molecule having a Michael acceptor or carbonyl group (s).View full abstractDownload PDF (419K) -
CHISAKO YAMAGAMI, MAKIKO SUGIURA, NARAO TAKAO1980 Volume 28 Issue 12 Pages 3665-3669
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe behavior of hydrochlorides and methiodides of several N-substituted 4-piperidones in CH3OH has been studied by 13C nuclear magnetic resonance (NMR) spectroscopy. All the piperidone salts studied were observed to exist as their hemiacetal form at room temperature, in contrast to the case of free piperidones, where an equilibrium mixture of ketone and hemiacetal was obtained. This difference could be accounted for by the effect of the positive charge on nitrogen, which increases the instability of the salt of the keto-form. Acetal formation was observed only in more acidic solutions. The corresponding O- and S-analogs were also examined in CH3OH, and it was found that they are converted readily to the acetals in the presence of trace amounts of acid. The reaction mechanisms of these compounds and piperidone salts are compared and discussed. 13C NMR techniques were found to be useful for studying the equilibrium system containing both hemiacetal and acetal.View full abstractDownload PDF (585K) -
KUNIO KOBAYASHI, KEIKO YOSHIDA, AKIRA MATSUOKA1980 Volume 28 Issue 12 Pages 3670-3673
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe D-[5-3H] glucose-binding membrane proteins in rat islet homogenate and its F2 fraction obtained by sucrose gradient (d20=1.00-1.18) ultracentrifugation at 70000g for 2 hr were analyzed by SDS-polyacrylamide gel electrophoresis. Five components in the F2 fraction, which contains membrane proteins related to glucose-induced insulin release, showed relative mobilities of around 0.75 on SDS gel stained with Coomassie brilliant blue (R-250), and had apparent molecular weights of 22000-30000. One component among them appeared to be a glycoprotein because it was sensitive to the periodic acid-Schiff reagent (PAS reagent).View full abstractDownload PDF (558K) -
TANEKAZU KUBOTA, KIYOSHI EZUMI1980 Volume 28 Issue 12 Pages 3673-3678
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe simultaneous determination of acid dissociation constants (pKa) and true partition coefficients (P) of a dibasic acid and a diacidic base was achieved by analyzing the pH dependence of the apparent partition coefficient (Pa). Equations derived theoretically show a parabolic relation of Pa to (H+)-1 and (H+) for a dibasic acid and a diacidic base, respectively, (H+) being the proton concentration. Theoretical considerations indicateView full abstractDownload PDF (707K) -
MAMORU FUKUMOTO1980 Volume 28 Issue 12 Pages 3678-3681
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBromazepam (7-bromo-1, 3-dihydro-5-(2-pyridyl)-2H-1, 4-benzodiazepin-2-one) was determined by formation the chelate compound with iron (II) followed by extraction from the organic phase into an aqueous solution. The absorption spectrum of the chelate compound in aqueous solution showed maximum absorbance at 580 nm and the absorbance was stable for about 5 hr at room temperature. The calibration curve was linear from 0.2 to 50 μg/ml of bromazepam and the sensitivity of the procedure was 0.2 μg/ml of bromazepam. This procedure was applied to the determination of bromazepam in rat blood. The recovery of added bromazepam from rat blood ranged from 96 to 100.5%, with a mean recovery of 99.1%.View full abstractDownload PDF (484K) -
SEIKI TANADA, KEITO BOKI, HITOSHI TAKAHASHI, TAKEO NAKAMURA1980 Volume 28 Issue 12 Pages 3681-3685
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdsorption of styrene on activated carbon was investigated on the basis of the adsorption isotherm, isosteric heat of adsorption, and compressed volume of condensed styrene. Regeneration of spent activated carbon was examined by the extraction of styrene with organic solvents. The Langmuir equation could be applied to the adsorption isotherms of styrene on activated carbon. The isosteric heats of adsorption of styrene on activated carbon Nos. 1-3 and 5-were less than twice the value of the heat of condensation of styrene (ΔH0=9.64 kcal/mol) in the range of θ 0.2 to 1.0, and therefore, styrene adsorbed in this range of θ seemed to be physisorbed on activated carbon. Styrene physisorbed on activated carbon seemed to be compressed in the pores. Spent activated carbon could be regenerated by extracting the styrene with acetone at about 30° and its adsorptive capacity became approximately equal to that of fresh activated carbon.View full abstractDownload PDF (597K) -
MUNEHISA ARISAWA, YUKO KYOZUKA, TOSHIMITSU HAYASHI, MINEO SHIMIZU, NAO ...1980 Volume 28 Issue 12 Pages 3686-3688
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNine isoflavonoids (I-IX) were isolated from the roots of Thermopsis fabacea D. C. (Leguminosae). The methanol extract afforded formononetin (I) and daidzein (II), the ethereal extract afforded trifolirhizin (III), dl-maackiain (IV), genistein (V), and 7, 3'-dihydroxy-4'-methoxyisoflavone (VI), and the ethyl acetate extract afforded formononetin-7-O-β-D-glucoside (VII), daidzin (VIII), and genistin (IX). These compounds were identified by means of degradation, spectroscopic studies, and direct comparison with authentic samples.View full abstractDownload PDF (499K) -
YOSHIAKI MUTO, HIROMI ICHIKAWA, KANAME TAKAGI1980 Volume 28 Issue 12 Pages 3688-3692
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSGuaiazulene (1, 4-dimethyl-7-isopropylazulene) reacted with malonyl dichloride in the absence of a Lewis acid to afford 3-(guaiazulen-3-yl)-3-oxopropionylchloride (1), which was converted by treatment with water into 3-(guaiazulen-3-yl)-3-oxopropionic acid (2) and 3-acetylguaiazulene (3). Upon treatment of 1 with some alcohols and aromatic amines, the corresponding esters (4) and amides (5) were obtained, respectively. The reaction of methyl 3-(guaiazulen-3-yl)-3-oxopropionate (4a) with hydrazine gave 3-(guaiazulen-3-yl)-3-oxopropionylhydrazide (6), which was easily cyclized into 5-(guaiazulen-3-yl)-2, 3-dihydropyrazol-3-one (7).View full abstractDownload PDF (633K) -
MASAYOSHI YAMAGUCHI1980 Volume 28 Issue 12 Pages 3693-3695
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of calcitonin (CT) and epinephrine on serum glucose concentration were investigated in fed rats. The administration of CT (80 MRC mU/100 g body weight) to adrenalectomized rats caused a significant increase in serum glucose. The simultaneous administration of CT (40 and 80 MRC mU/100 g) and epinephrine (7.5 and 15 μg/100 g) produced a clear increase in comparison with that caused by epinephrine alone. On the other hand, CT did not change the glucose tolerance, while epinephrine markedly lowered it. The present results suggest that the hyperglycemic effect caused by CT is not mediated through the action of epinephrine from adrenal glands in rats.View full abstractDownload PDF (430K) -
TAKEHIKO YAJIMA, TOSHIHIKO ITOH, SATOSHI MUTOH, HIDETAKA YUKI1980 Volume 28 Issue 12 Pages 3696-3698
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new polyacrylamide gel electrophoretic system with post-labeling of proteins with o-phthalaldehyde (OPT) has been developed. In the present system, the widely used tris, glycine and ammonium persulfate were replaced by triethanolamine, L-hydroxyproline and sodium persulfate, respectively. Proteins were visualized by dipping the gels in the OPT reagent for several minutes immediately after electrophoresis, and the gels were then scanned in a fluorescence densitometer. Fifty nanograms of bovine serum albumin could be detected by this technique.View full abstractDownload PDF (437K) -
SHIRO YOSHIZAKI, EIYU YO, KAZUYUKI NAKAGAWA, YASUMITSU TAMURA1980 Volume 28 Issue 12 Pages 3699-3701
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 5-(2-allylamino-1-hydroxyalkyl)-8-hydroxycarbostyrils (4) was synthesized. The β-adrenoceptor stimulant activities of erythro-5-(2-allylamino-1-hydroxypropyl)-8-hydroxycarbostyril (4b) in anesthetized dogs were determined.View full abstractDownload PDF (428K) -
TETSURO NAGASAWA, JINHO CHOI, YOSHIE NISHINO, HIKOKICHI OURA1980 Volume 28 Issue 12 Pages 3701-3707
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe minor components of ginseng saponins, ginsenoside-Rf, -Rg2, and -Rh1, were isolated from the crude saponin fraction by a high-performance liquid chromatography (HPLC) procedure involving preparative HPLC on silica gel followed by semi-preparative HPLC on a column packing of Carbohydrate Analysis. This method was rapid and convenient.View full abstractDownload PDF (653K) -
HIROTERU SAYO, KOICHI MORI, TAKASHI MICHIDA1980 Volume 28 Issue 12 Pages 3707-3710
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSConstant current electrolysis of 4'-substituted 2-nitrobenzenesulfenanilides (4'-OMe (1a), 4'-Me (1b), 4'-Cl (1c), 4'-COOEt (1d)) was carried out in acetonitrile containing 0.1 M ethyltributylammonium trifluoromethanesulfonate (ETBT), 1% trifluoroacetic acid, and 1% trifluoroacetic anhydride at a reticulated vitreous carbon (RVC) electrode. The quantity of electricity to be fed into the electrolytic cell was determined from the anodic potential-time curves. The yields of 2, 7-disubstituted phenazines (di-OMe (2a), di-Me (2b), di-Cl (2c), di-COOEt (2d)) were 56%, 24%, 42%, and 33%, respectively. The RVC anode was found to be useful for preparative electrolysis of 1a-d, since the considerable yields of phenazines were obtained within several minutes without the use of an expensive potentiostat.View full abstractDownload PDF (517K) -
KO KANEKO, NOBUAKI NARUSE, MIKAKO TANAKA, NAOTOSHI YOSHIDA, HIROSHI MI ...1980 Volume 28 Issue 12 Pages 3711-3713
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFritillarizine (22S, 25S)-cev-5-enine-3α, 20β-diol, a new Fritillaria alkaloid was isolated from the hydrolysis products of aerial part extracts of mature Fritillaria verticillata and its structure and absolute configuration were determined by conversion from verticinone.View full abstractDownload PDF (402K) -
TAKASHI YOSHIDA, RITSUSHI FUJII, TAKUO OKUDA1980 Volume 28 Issue 12 Pages 3713-3715
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures of chebulinic acid and chebulagic acid, which were previously formulated as dicarboxylic acids, Ib and IIb, have been revised to monocarboxylactones, Ic and IIc, respectively, on the basis of spectral and chemical evidences.View full abstractDownload PDF (371K) -
HIROSHI KASHIWAGI, SABURO ENOMOTO1980 Volume 28 Issue 12 Pages 3716-3718
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSStable free radical formation was observed in the binary powders of silicates and general organic compounds by the use of ESR at room temperature in the air. A large amount of free radicals was formed, if an OH or COOH group containing organic molecule was used. Free radicals were stable not only in the air but also in the suspension of benzene. However, they disappeared immediately upon contact with proton donating liquid molecules. Increase in spectral intensities with time and variation of spectral shapes with moisture were observed.View full abstractDownload PDF (466K) -
TETSUO NAGANO, KUMI ARAKANE, MASAAKI HIROBE1980 Volume 28 Issue 12 Pages 3719-3721
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSuperoxide (O2-) generated by crown ether/KO2 or electrochemical method undergoes epoxidation of olefins in the presence of acyl halide of benzenesulfonyl chloride. The reaction mechanisms are also discussed.View full abstractDownload PDF (439K) -
NAOKI MIYATA, KIYOKO UBA, KEIZO WATANABE, MASAAKI HIROBE1980 Volume 28 Issue 12 Pages 3722-3724
Published: December 25, 1980
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMorphine-7, 8-oxide (1) was synthesized from 3-methoxymethylmorphinone-7, 8-oxide which was obtained by the oxidation of 3-methoxymethylmorphinone with H2O2. Heroin-7, 8-oxide (2) was also synthesized from 1. The analgesic activity of 7, 8-epoxides (1, 2 and codeine-7, 8-oxide) was determined by the method of pressure stimuli on the rat tail. 2 was the most analgesic among all of them. In comparison with each of their parent compound (morphine, heroin and codeine), the introduction of the 7, 8-epoxy moiety into morphine skeleton resulted in some increase in their analgesic activity.View full abstractDownload PDF (361K)
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