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Koji MIURA, Ikuko OKADA
1965 Volume 13 Issue 5 Pages
525-528
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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Sixteen nitrofurylvinylquinoline compounds were examined for their phage inducing activity on E. coli K 12 (λ), a lysogenic strain. Excepting compounds having -COOH, -CONH
2, -NO
2, or -Br on the quinoline nucleus, they had phage inducing ability. The compound, 4, 6-Diamino-2Q-ran HCl was the strongest among them and its activity was twice as strong as that of Mitomycin C, a drug for cancer. It is a notable fact that the tested nitrofurylvinylquinoline compounds which have an inducing activity in lysogenic bacteria exhibit, with one exception, an antitumor effect on bearing Ehrlich ascites carcinoma.
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koji Miura, Masao Ikeda, Tomiji Oohashi, Yoshiko Igarashi, Ikuko Okada
1965 Volume 13 Issue 5 Pages
529-534
Published: May 25, 1965
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Six methylol derivatives of nitrofurylvinylogues were prepared from their parent compounds with formaldehyde or paraformaldehyde in water or in organic solvents. Of these, antitumor effect on Ehrlich ascites carcinoma in mice was investigated. 2-Bis(hydroxymethyl)amino-4-[2-(5-nitro-2-furyl) vinyl] pyrimidine (D-ran-methylol) and 2-bis(hydroxymethyl)amino-4-[2-(5-nitro-2-furyl) vinyl] quinoline (2A-4Q-ran-methylol) were revealed to save mice completely from tumor death with the suitable dose intraperitoneally. These two compounds had small toxicities and administrations of 1, 000 mg. per kilo did not kill any mouse.
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Tsutomu Momose, Yosuke Ohkura, Kazuya Kohashi
1965 Volume 13 Issue 5 Pages
534-538
Published: May 25, 1965
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A simple method has been presented for the determination of 3-hydroxybutyric acid in blood. It is based on the oxidation of 3-hydroxybutyric acid to acetone with potassium dichromate in sulfuric acid, which is distilled during the oxidation and determined by the previously established method with trinitrobenzene as a color developing agent. Simple and compact oxidation-distillation equipment has been designed and successfully used, which made possible to analyze many samples at the same time.
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Masao Tomita, Toshiro Ibuka, Yasuo InubushiI, Yasuo Watanabe, Matao Ma ...
1965 Volume 13 Issue 5 Pages
538-545
Published: May 25, 1965
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The structure of hasubanonine was reexamined and the complate constitution (IIc) including the absolute stereostructure was presented. The structure of homostephanoline was also investigated and three possible structure for this alkaloid were shown in formulae (XIIIa), (XIIIb), (XIIIc). These two alkaloids have a novel skeleton (XII) which has not been known hitherto in the natural sources, for which the name "hasubanan" was proposed.
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Tameto Okanishi, Akira Akahori, Fumio Yasuda
1965 Volume 13 Issue 5 Pages
545-550
Published: May 25, 1965
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From the aerial parts of Smilax sieboldi MIQ. a new steroidal sapogenin, laxogenin (I), was isolated together with tigogenin and neotigogenin. The analytical values of I corresponded to formula C
27H
42O
4 for sapogenin and C
29H
44O
5 for the acetate. On Huang-Minlon reduction I afforded tigogenin (II), and on sodium borohydride reduction of I, β-chlorogenin (III) and chlorogenin (IV) were obtained in ratio about 85 : 15. The chromic acid oxidation of I afforded a diketone (V), m.p. 229∼231°, which was proved to be identical with 25
D-allospirostane-3, 6-dione. From these results the structure of laxogenin was assumed to be 3β-hydroxy-25
D, 5α-spirostan-6-one and this assumption was confirmed by the synthesis of this compound from 5, 6-epoxydiosgenin (XI).
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Kiichiro Kakemi, Takaichi Arita, Hitoshi Sezaki, Norio Takasugi
1965 Volume 13 Issue 5 Pages
551-557
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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1) The stability of sodium (2-isonicotinoylhydrazino) methanesulfonate in isotonic buffer solutions at 37° was found to be stable at low and relatively unstable at neutral pH regions. 2) The stability of isonicotinoyl hydrazones was found to decrease with lowering pH. The facile degradation of these compounds in the stomach should be taken into cosideration for oral administration. 3) Isoniazid was absorbed poorly from the stomach, and rapidly from the intestine. Sodium (2-isonicotinoylhydrazino)methanesulfonate was absorbed more slowly from the stomach and the intestine. 4) Intestinal absorption patterns of isonicotinoylhydrazones were divided into two groups ; slow and rapid ones. Glucose, lactose, glucuronolactone, and sodium pyruvate isonicotinoylhydrazones were hardly absorbed in intact form whereas furyl methyl ketone isonicotinoylhydrazone was absorbed in intact form to a considerable extent. There was a rough relationship between the degree of absorption of these hydrazones and their lipid/water partition characteristics. 5) The fact that intact hydrazones of slow absorptive group are poorly absorbed was further demonstrated by the urinary excretion study using glucose isonicotinoylhydrazone by humans. 6) Suggestion was obtained to use isonicotinoylhydrazones belonging to rapid absorption group effectively by stabilization of the drug in the gut.
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Yoshihiro Nitta, Kiyoshi Okui, Kiyohiko Ito
1965 Volume 13 Issue 5 Pages
557-567
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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The synthesis of a number of sulfonamides having dialkylamino groups in the pyrimidine nucleus was described. Among these new compounds, N
1-(6-chloro-2-dialkylamino-4-pyrimidyl)sulfanilamide were found to possess notable antibacterial activities.
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Yoshihiro Nitta, Kiyoshi Okui, Kiyohiko Ito, Mitsuhisa Togo
1965 Volume 13 Issue 5 Pages
568-573
Published: May 25, 1965
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Nous avons effectue le synthese des(alcoxy-2-pyrimidyl-4)-N
1-sulfanilamides. La condensation des amino-4-alcoxy-2-pyrimidines avec le chlorure de p-nitro-benzenesulfonyle est tres difficile, surtout la (methoxy-2-pyrimidyl-4)-N
1-sulfanilamide n'est pas obtenue par cette methode, donc elle a ete preparee par l'autre methode et possede l'activite antibacterienne intense.
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Fumio Yoneda, Yoshihiro Nitta
1965 Volume 13 Issue 5 Pages
574-579
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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The relation between the electronic structure and the local anesthetic activity of 2-diethylaminoacetanilide derivatives was investigated by a molecular orbital method and it was found that the stabilization energy due to the charge transfer complex formation between these compounds and thiamine has something to do with their local anesthetic activities.
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Fumio Yoneda, Takayuki Ohtaka, Yoshihiro Nitta
1965 Volume 13 Issue 5 Pages
580-585
Published: May 25, 1965
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3, 4, 5-Trichloropyridazine on treatment with 2-aminothiophenol gave 4-chloro-10H-benzo[b]pyridazino[3, 4-e][1, 4]thiazine (II) and 1-chloro-10H-benzo[b]pyridazino[4, 5-e][1, 4]-thiazine (III). II was converted into 10H-benzo[b]pyridazino[3, 4-e][1, 4]thiazine by catalytic dechlorination. Treatment of 4, 5-dichloro-3-(2H)-pyridazinone with 2-aminothiophenol afforded 5-(2-aminophenylthio)-4-chloro-3(2H)pyridazinone, which was cyclized on heating with potassium carbonate in dimethylformamide to yield 10H-benzo[b]pyridazino[4, 5-e][1, 4]thiazin-1(2H)-one. Chlorination of the latter with phosphoryl chloride and N, N-dimethylaniline afforded III. Several 2-substituted-10H-benzo[b]-pyridazino[4, 5-e][1, 4]thiazin-1(2H)-ones were synthesized.
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Yoshihiro Nitta, Ikutoshi Matsuura, Fumio Yoneda
1965 Volume 13 Issue 5 Pages
586-593
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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5, 8-Dichloropyrido[2, 3-d]pyridazine was prepared and its reactions with nucleophiles, such as hydroxide, alkoxide, thiourea, ammonia, anilines, and hydrazine were carried out. Monosubstituted isomeric products were isolated, and their isomeric structures were determined by converting them into known structures. Monohydrazino derivatives were cyclized with acid or acid anhydride into triazolo derivatives.
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Yoshio Sakurai, Eiichi Matsui
1965 Volume 13 Issue 5 Pages
594-598
Published: May 25, 1965
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A number of new amide derivatives of bis(2-chloroethyl)-DL-glycine and bis(2-chloroethyl)-DL-alanine were prepared and tested for their in vivo and in vitro antitumor activity against Yoshida Sarcoma, and chemical properties.
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Shoshiro Nakamura, Takeo Chikaike, Hiroshi Yonehara, Hamao Umezawa
1965 Volume 13 Issue 5 Pages
599-602
Published: May 25, 1965
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3-Methyl-3-phenyl-L-alanine, L-2-amino-3, 3-dimethylbutyric acid, L-valine, cis-3-methyl-L-proline, 3-(2-thiazolyl)-β-alanine and glycine are isolated from hydrochloric acid hydrolyzate of bottromycin A. Characterization and structural studies of the new amino acids, L-2-amino-3, 3-dimethylbutyric acid and cis-3-methyl-L-proline, are described.
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J.D. Connolly, Yoshio Kitahara, K.H. Overtion, Akira Yoshikoshi
1965 Volume 13 Issue 5 Pages
603-605
Published: May 25, 1965
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It is proved by direct comparison that the nor-ketone (VIIa) derived from dolabradiene was enantiomeric with those (VIIb) from erythroxydiol Y. This is a further confirmation on configuration at C
13 of dolabradiene and erythroxydiol Y.
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Satoshi Toki, Tamiko Takenouchi
1965 Volume 13 Issue 5 Pages
606-609
Published: May 25, 1965
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α-3-OH-HB-GA was isolated from the urine of rabbit administered hexobarbital. The position of the conjugated glucuronic acid was suggested by ultraviolet absorption spectrum, and the structure of aglycone was confirmed by enzymatic and acid hydrolysis.
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Tadashi Okabayashi, Misao Ide, Akihiro Yoshimoto, Miyuki Otsubo
1965 Volume 13 Issue 5 Pages
610-611
Published: May 25, 1965
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Koroku Hashimoto, Fumihiko Yoshida
1965 Volume 13 Issue 5 Pages
612-613
Published: May 25, 1965
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Molsin increased the growth rate of rats without any toxicities, when added in doses of 0.05 and 0.5% to the basal diet. The incidence of death resulting from pneumonia was found significantly less in Molsin groups than in the control.
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Bunji Shimizu, Motoji Asai, Harukiyo Hieda, Michiko Miyaki, Hiroshi Ok ...
1965 Volume 13 Issue 5 Pages
616-618
Published: May 25, 1965
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Eiji Ochiai, Makoto Takahashi
1965 Volume 13 Issue 5 Pages
618-622
Published: May 25, 1965
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Naoto Yoneda
1965 Volume 13 Issue 5 Pages
622-625
Published: May 25, 1965
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Hiroshi Hikino, Yasuyoshi Takeshita, Yasuko Hikino, Tsunematsu Takemot ...
1965 Volume 13 Issue 5 Pages
626-628
Published: May 25, 1965
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Hiroshi Hikino, Keitaro Aota, Tsunematsu Takemoto
1965 Volume 13 Issue 5 Pages
628-630
Published: May 25, 1965
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Hiroshi Hikino, Yasuyoshi Takeshita, Yasuko Hikino, Tsunematsu Takemot ...
1965 Volume 13 Issue 5 Pages
631-632
Published: May 25, 1965
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Shinsaku Natori, Yuko Kumada, Hidejiro Nishikawa
1965 Volume 13 Issue 5 Pages
633-635
Published: May 25, 1965
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Zen-ichi Horii, Takefumi Momose, Yasumitsu Tamura
1965 Volume 13 Issue 5 Pages
635-636
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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Zen-ichi Horii, Masami Makita, Ikuko Takeda, Yasumitsu Tamura, Yoshiak ...
1965 Volume 13 Issue 5 Pages
636-638
Published: May 25, 1965
Released on J-STAGE: March 31, 2008
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