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Volume 8, Issue 2
Displaying 1-22 of 22 articles from this issue
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Morizo Ishidate, Shigeru Tsukagoshi1960 Volume 8 Issue 2 Pages 87-89
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-Methyl[14C]-bis(2-chloroethyl)amine N-oxide (14C-labeled nitrogen mustard N-oxide) was synthesized for pharmacological and biochemical experiments using Methyl-[14C]iodide. Its specific activity was determined as 6, 500 counts/min./μmole by Q-gas flow counter. The labeled compound was given to a dog intravenously and the urine was taken out from the opened bladder. Concentration of the compound in the urine was quantitatively determined by radioactivity measurement.View full abstractDownload PDF (419K) -
Morizo Ishidate, Yoshio Sakurai, Eiichi Matsui1960 Volume 8 Issue 2 Pages 89-94
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEach of 10 different derivatives of nitrogen mustard was tested on 12 Yoshida sarcoma rats for their life-prolongation and leucopenia-inducing effects. It was found that some showed a very strong effect of life-prolongation on the tumor rats, although the leucopenia-inducing effect of such compounds was quite equal to those of other compounds.View full abstractDownload PDF (501K) -
Morizo Ishidate, Yoshio Sakurai, Eiichi Matsui1960 Volume 8 Issue 2 Pages 95-98
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBis(diphenylphosphate) of N-emthyl- and N-phenyl-bis(2-hyproxyethyl)amine was proved to have alkylating activity against mercapto group of L-cysteine and thiosulfate in a neutral aqueous solution. The compounds exhibited only a slight anti-tuomr cytological effect on Yoshida sarcoma in vitro and in vivo.View full abstractDownload PDF (533K) -
Morizo Ishidate, Yoshio Sakurai, Isao Aiko1960 Volume 8 Issue 2 Pages 99-103
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwenty new derivative of nitrogen mustard, including six N-oxides, were prepared and tested for their in vivo and in vitro antitumor activity against the Yoshida.View full abstractDownload PDF (593K) -
Ryuichi Kimura, Takahiro Yabuuchi, Yasutaka Tamura1960 Volume 8 Issue 2 Pages 103-107
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs some thiophene derivatives have interesting pharmacological action, 2-aminoethyl 3, 3-diaryl-3-hydroxypropanoates and 2-aminoethyl 3, 3-diaryl-2-propenoates having thiophene ring were synthesized. Esterification of3, 3-diaryl-3-hydroxypropanoic acids, prepared by the Reformatsky reaction of diaryl ketones, and 3, 3-diaryl-2-propenoic acid prepared by dehydration of these hydroxypropanoic acid gave aminoethyl esters of the corresponding acids.View full abstractDownload PDF (546K) -
Masao Shimizu, Genkichi Ohta1960 Volume 8 Issue 2 Pages 108-111
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOryzanol-B was shown to be largely a mixture of cycloart-24-enyl ferulate (oryzanol-A) and 24-methylenecycloartanyl ferulate (oryzanol-C) by comparison of melting points of their derivatives and by degradation. Alcohol-B, obtained by saponification of oryzanol-B, was acetylated and ozonolysis of acetate afforded 24-oxocycloartanyl acetate and 3β-acetoxy-25, 26, 27-trisnorcycloartan-24-oic acid. Comparison of alcohol-B with reported triterpenes of rice-bran oil is described.View full abstractDownload PDF (591K) -
Masao Uchibayashi1960 Volume 8 Issue 2 Pages 112-116
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMicrobiological transformation of Reichstein's Substance S (I) by Pseudomonas sp. 109 afforded hydrocortisone (IV) and 17α, 20β, 21-trihydroxy-1, 4-pregnadien-3-one (II), and structure of the latter was verified.View full abstractDownload PDF (647K) -
Masao Uchibayashi1960 Volume 8 Issue 2 Pages 117-121
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMicrobiological transformation of Reichstein's Substans S (I) to 17α, 20β, 21-trihydroxy-1, 4-pregnadien-3-one (II) and 17α, 21-dihydroxy-1, 4-pregnadiene-3, 20-dione (III) by the action of Pseudomonas sp. 125, and to 17α, 20β, 21-trihydroxy-4-pregnen-3-one (IV) by Pseudomonas sp. M8 was described.View full abstractDownload PDF (673K) -
Masao Uchibayashi1960 Volume 8 Issue 2 Pages 122-125
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSodium borohydride reduction of Reichstein's Substance S (I) furnished 17α, 20β, 21-trihydroxy-4-pregnen-3-one (II) and 4-pregnene-3β, 17α, 20β, 21-tetrol (IV), and the structure of the latter was verified. Selective oxidation by N-bromoacetamide converted compound (IV) into (II) and catalytic hydrogenation of compound (V) was accompanied by hydrogenolysis to afford the triacetate (VI) of Reichstein's Substance K and 20β, 21-diacetoxyallopregnan-17α-ol (VIII), which was led to the free steroid (VII) for identification.View full abstractDownload PDF (585K) -
Eiji Ochiai, Chikara Kaneko, Iwao Shimada, Yumiko Murata, Takuo Kosuge ...1960 Volume 8 Issue 2 Pages 126-130
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS6-Nitrochinolin ergab bei der Oxydierung mit Wasserstoffperoxyd in einer Eisessig-Losung das entsprechende N-Oxyd nur in einer Ausbeute von 41% und nebenbei entstanden 3-Hydroxy-6-nitrochinolin und sein N-Oxyd in einer Ausbeute von 1% bzw. 27% der Theorie. Die analoge Reaktion mit chinolin-8-carbonsaure bzw. Seinem Athylester ergab kein N-Oxyd sondern das entsprechende 3-Hydroxyderivat in einer Ausbeute von 36% bzw. 21% der Theorie. Die Nebenentstehung von 3-Hydroxyderivat bei der N-Oxydierung eines Chinolinderivates mit Wasserstoffperoxyd in Eisessig-Losung scheint eine allgemeine Erscheinung zu sein, die bei der sterischen oder polarischen Hinderung durch irgendeinen Substituenten deutlicher auftritt.View full abstractDownload PDF (725K) -
Morizo Ishidate, Hidetaka Yuki1960 Volume 8 Issue 2 Pages 131-136
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHeating of the sodium salt of 4-amino-5-acylamino-6-mercaptopyrimidine results in the formation of a purine derivative but its heating with dilute hydrochloric or sulfuric acid was found to give thiazolo[5, 4-d]pyrimidine derivatives. 5-Amino-6-mercaptopyrimidine derivatives react with nitrile to form thiazolo[5, 4-d]pyrimidine derivatives, while they react with monochloroacetic acid to form pyrimido[4, 5-b][1, 4]thiazine derivatives, and with nitrous acid to form thiadiazolo[5, 4-d]pyrimidine derivatives.View full abstractDownload PDF (711K) -
Rearrangement Reaction of 7-Mercaptooxazolo[5, 4-d]pyrimidine to 7-Hydroxythiazolo[5, 4-d]pyrimidineMorizo Ishidate, Hidetaka Yuki1960 Volume 8 Issue 2 Pages 137-139
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS7-Mercapto-2-methyloxazolo[5, 4-d]pyrimidine was found to undergo rearrangement to 7-hydroxy-2-methylthiazolo[5, 4-d]pyrimidine either by boiling with dilute hydrochloric acid or by heating the crystals to 270∼300°.View full abstractDownload PDF (425K) -
Makoto Miyazaki, Mieko Hashi, Tyunosin Ukita1960 Volume 8 Issue 2 Pages 140-146
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3-(1-Hydroxyethyl)-S-guaiazulene (III) was prepared by reduction of 3-acetyl-S-guaiazulene (II) with lithium aluminum hydride. (III) was converted into 3-vinyl-S-guaiazulene (IV) by dehydration and further into 3-ethyl-S-guaiazulene (V) by catalytic hydrogenation. An isomeric carbinol (VIII) was also produced from S-guaiazulene-3-carboxaldehyde (VI) by its treatment with methylmagnesium iodide, and (VIII) was confirmed to be 3-(1-hydroxyethyl-S-guaiazulene by its derivation to (V). The remarkably different stability against dehydration observed between the two isomeric 3-(1-hydroxyethyl)-S-guaiazulenes (III and VIII) is discussed from the structural point of view.View full abstractDownload PDF (783K) -
Makoto Miyazaki1960 Volume 8 Issue 2 Pages 146-149
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe Schiff bases, N-(S-guaiazulen-3-ylmethylene)cyclohexylamine (II), N-(S-guaiazulen-3-ylmethylene)benzylamine (III), and N-(S-guaiazulen-3-ylmethylene)-1, 1-dimethyl-2-hydroxyethylamine (IV) were prepared in excellent yields by condensation of S-guaiazulene-3-carboxaldehyde (I) with corresponding primary amines. These bases were easily converted into secondary amino derivatives of S-guaiazulene, i.e. 3-cyclohexylaminomethyl-S-guaiazulene hydrochloride (VIII), 3-benzylaminomethyl-S-guaiazulene hydrochloride (IX), and 3-(1, 1-dimethyl-2-hydroxyethylaminomethyl)-S-guaiazulene hydrochloride (X), by catalytic hydrogenation and salt formation with hydrochloric acidView full abstractDownload PDF (497K) -
Hyozo Taniyama, Shoji Takemura1960 Volume 8 Issue 2 Pages 150-153
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new streptothricin-like antibiotic, racemomycin-O, obtained from the fermented broth of Streptomyces racemochromgenus novo sp.(Shinobu-strain), was examined. The isolation and purification of this antibiotic as a picrate is described and some physical and chemical properties and presented. It was shown that analytical and molecular weight determinations of free base and various salts agreed with the molecular formula of C25H44O10N8. Racemomycin-O is a nontoxic antibiotic while racemomycin-B has a strong toxicity.View full abstractDownload PDF (511K) -
Shoji Takemura1960 Volume 8 Issue 2 Pages 154-156
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs the degradation products of recemomycin-O, β-lysine (I), roseonine (II), and D-glucosamine (IV) were obtained. β-Lysine and roseonine were isolated as picrates and the amino sugar was identified by paper chromatography and isolated as N-benzoyloxycarbonyl derivative which was identical with the authentic N-benzoyloxycarbonyl-D-glucosamine in mixed melting point and optical rotations.View full abstractDownload PDF (411K) -
Tadashi Okabayashi, Hideo Kano, Yasuo Makisumi1960 Volume 8 Issue 2 Pages 157-162
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSixty-eight substituted azaindolizines were tested for their activity on Lactobacillus casei and Streptococcus faecalis. These azaindolizines could be divided into three classes according to the pattern of growth inhibition, substituent present, and the position of the substituent in azaindolizine molecule. Compounds in Group 1 and 2 which have sulfurcontaining substituents and halogen groups, respectively, were not affected appreciably by folic acid, leucovorin, thymine, or purines, while Group 2 compounds which have amino or closely related groups were antagonized by folic acid, leucovorin, and thymine but not by purines.View full abstractDownload PDF (562K) -
Tadashi Okabayashi1960 Volume 8 Issue 2 Pages 162-167
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHalogenated azaindolizines were found to inhibit the growth of E. coli strains in saltglucose medium and to have the inhibition reversed by tyrosine or some other amino acids. Compounds which were most inhibitory and most prominently reversed by tyrosine were those that have two halogen groups in 5- adn 6-positions of the azaindolizine molecule. The activity of compounds that have only one halogen substituted in 5-position was much smaller than that of dihalogenated compounds. Most of the compounds that have only one halogen in 6-position did not exert any inhibiton on the growth of E. coli.View full abstractDownload PDF (557K) -
Eiichi Matsui1960 Volume 8 Issue 2 Pages 168-169
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSdl-Octadecyl α-glyceryl ether (batyl alcohol) was synthesized and tested for its inhibiting action on the rat leucopenia induced by administration of N-methyl-bis(2-chloroethyl)amine N-oxide.View full abstractDownload PDF (328K) -
Takahiro Tabuuchi1960 Volume 8 Issue 2 Pages 169-172
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs some thiophene derivatives have interesting pharmacological actions, some new 3-arylpropenamides having thiophene ring were synthesized. The reactions of amines and 3-arylpropenoyl chloride, which were synthesized from 3, 3-di(2-thienyl)-3-hydroxypropionic acid, 3-phenyl-3-(2-thienyl)-3-hydroxypropionic acid, or 3-(2-thienyl)propenoic acid with thionyl chloride, gave the corresponding derivatives of propenamides.View full abstractDownload PDF (511K) -
Goro Chihara, Ayako Mizushima, Kimiko Shirakuma, Yutaka Mizushima, Tak ...1960 Volume 8 Issue 2 Pages 173-174
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (494K) -
Goro Chihara, Kimiko Shirakuma, Ayako Mizushima, Emiko Kobayashi1960 Volume 8 Issue 2 Pages 174-176
Published: February 25, 1960
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (521K)
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