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Volume 12, Issue 2
Displaying 1-19 of 19 articles from this issue
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Yuichi Kanaoka, Takamitsu Sekine, Minoru Machida, Yaeko Soma, Kazutaka ...1964 Volume 12 Issue 2 Pages 127-134
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN- [(4(or 7)-Methoxy-2-benzimidazolyl) methyl] maleimide (IIIa) was synthesized as"fluorescence-labeled"protein-sulfhydryl reagent. Polyphosphoric acid was proposed to be a general reagent for imide cyclization reaction. Fluorescent characteristics of some benzimidazole derivatives were described.View full abstractDownload PDF (854K) -
Keiji Sekiguchi, Noboru Obi, Yoshio Ueda1964 Volume 12 Issue 2 Pages 134-144
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermal analyses of the system of chloramphenicol and urea were carried out both by the thaw-melt and the DTA method. The system gave a phase diagram of simple eutectic type. The eutectic mixture melts at 104°and has a composition of 76% of the antibiotics and 24% of urea by weight. Dissolution rates of ordinary chloramphenicol, and four kinds of samples prepared by mechanical mixing or by fusion of both substances were investigated. Although the eutectic mixture itself did not dissolve rapidly, the fused conglomerate having a weight ratio of 1 : 4 dissolved much more rapidly, and a maximum was observed in its dissolution curve. Such a peculiar dissolution can be attributed to the size reduction of chloramphenicol by the formation of eutectic mixture and the presence of easily soluble primary crystals of urea which have much greater surface available for contact with the surrounding solution. When the fused conglomerate of this composition was administered to rabbits in suspension or capsule form, the antibiotics was absorbed much more rapidly and to a greater extent. High correspondence between dissolution and absorption rate indicates that the absorption of chloramphenicol is largely dependent on the rate of dissolution which is intimately related to the physical state. It is thought that this new form of medication will be effectively applied for therapeutical purpose, when blood concentration should be achieved as rapidly as possible and yet patients can not receive the antibiotics by injection.View full abstractDownload PDF (965K) -
Morio Ikehara, Eiko Ohtsuka, Yoshihiro Kodama1964 Volume 12 Issue 2 Pages 145-150
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhosphorylation of adenosine with morpholino phosphorodichloridate, P1-diphenyl P2-morpholino pyrophosphorochloridate and 2, 6-lupetidyl phosphorodichloridate in the presence of boric acid was performed in DMF solution. It was observed that the ratio of resulting 5'-monophosphate to 2'-+3'-monophosphate was in the range of 2.7∼5.5, which indicated the protection of borate complex on 2'-and 3'-hydroxyl group of adenosine against the attack of the phosphorylating agent.View full abstractDownload PDF (651K) -
Masayasu Kimura1964 Volume 12 Issue 2 Pages 150-159
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to determine the site of action of organophosphate group on acetylcholine (ACh) receptor surface, the effect of several antagonists of ACh has been observed with Magnus method using the isolated intestine of mice. These experiments gave following results : 1) A modified method for determining the site of action of antagonist on ACh receptor surface was established stochastically and the validity was evidenced by two trial experiments. 2) According to this justified method, the anticholinergic effect of four pairs consisting of two antagonists were demonstrated and from these results, four pairs were divided into groups acting on the same site and on the different site ; the former is two pairs consisting of pyridine aldoxime methiodide (PAM) and atropine, and parathion and isopentyl acetate, the latter is two pairs consisting of atropine and parathion, and parathion and PAM. From this fact, it was concluded that organophosphate group of parathion is attracted to, what is called, the esteratic site of ACh receptor surface in the inhibitory action against ACh. 3) From the fact that the interaction between PAM and butyl diethyl phosphate is recognized but PAM and isopropyl phosphate are independent each other in the inhibitory action against ACh, it was suggested as the possible mechanism that the butyl radical of phosphate can be to hinder the approach of PAM to the anionic site of ACh receptor surface. This is an experimental evidence that there are two active sites with the distance of 7 A on ACh receptor surface.View full abstractDownload PDF (859K) -
Masayasu Kimura, Isamu Saikawa1964 Volume 12 Issue 2 Pages 159-165
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo clarify the relationship between anticholinergic and anticholinesterase (anti-ChE) activities on the basis of chemical structure, nineteen organophosphoryl choline derivatives [chemical formula] were synthesized. Curare-like, atropine-like and anticholinesterase actions of these compounds were tested to screen. The experimental results were as follows : 1) Curare-like and atropine-like actions were both studied by Magnus method, observing their effect on rectus abdominis of frog and on intestines of white mice. Anti-ChE action on enzyme preparation from rabbit serum was tested by using Warburg's manometric method. 2) As to the basic structure of various organophosphoryl choline derivatives, curarelike action was increased in the following order of magnitude ; [chemical formula]. The R radicals increased the potency in the following order ; [chemical formula] and as for quaternary ammonium salts of derivatives, bromides were more potent than iodides. From these compounds it was found that four derivatives of NP-244 (I), NP-245 (I), NP-244pC (I) and NP244pB (I) was more potent than curare. 3) On the atropine-like action of organophosphoryl choline derivatives, the relation between their structure and potency was found to have the same tendency as in the case of curare-like action, but all of these derivative were weaker than that of atropine. 4) On the anti-ChE action of organophosphoryl choline, the basic structures increased its potency in the following order ; [chemical formula], but the change in R radicals did not always increase the potency of their curare-like action. All of these derivatives were weaker than neostigmine. 5) The relationship between curare-like and atropine-like actions and between curare-like and anti-ChE actions were discussed with the selective indexes calculated from experimental results. Some of thionothiol-phosphate have both curare-like and ChE activity, and its curare-like action is little antagonized by neostigmine. From these facts, it was suggested that acetylcholine receptor was perhaps different from ChE.View full abstractDownload PDF (736K) -
Yukio Akahori, Seigo Fukushima1964 Volume 12 Issue 2 Pages 166-175
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSKinetic study of isotope exchange reaction between p-nitrophenyl acetate and acetic anhydride in pyridine showed that one half of the radioactivity of acetic anhydride was employed for the exchange reaction. The result agreed with that of exchange reaction between acetic acid and p-nitrophenyl acetate, and the reaction showed exact linearity of log (1-F) vs. t. The exchange rate N was shown to be the first order function with respect to the ester and the acid. From the experiments carried out at 45.0°, 37.0°, 25.5°, and 0°, 14.7 kcal./mole was estimated for Ea. The mechanism, nucleophilic attack of acetoxyl group to the positive center of carbonyl group in the ester followed by acyloxygen fission, was considered to be most probable.View full abstractDownload PDF (957K) -
Yoshifumi Maki, Kazunaga Obata1964 Volume 12 Issue 2 Pages 176-182
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe behaviors of various 4, 5-di-and 3, 4, 5-trisubstituted 1-phenyl-6 (1H)-pyridazinone against caustic alkali and hydrobromic acid were investigated. From these data, the mechanism of the ring-contraction from pyridazinone to pyrazolone, as shown in Chart 1, was discussed. Action of 1-phenyl-4, 5-dichloro-6 (1H)-pyridazinone with boiling caustic alkali took place the ring-contraction to give unexpected 1-phenyl-3-hydroxy-5-pyrazole-carboxylic acid. The mechanism of this reaction was also assumed as shown in Chart 4. Moreover, the reactivity of chlorines on 1-phenyl-3, 4, 5-trichloro-6 (1H)-pyridazinone was elucidated to increase in the order 4-, 5-, 3-position from the result of its methoxylation reaction.View full abstractDownload PDF (766K) -
Jiro Kinugawa, Michihiko Ochiai, Chikashi Matsumura, Hiroichi Yamamoto1964 Volume 12 Issue 2 Pages 182-191
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Alkoxythiocarbonylthio-and 4- (N, N-disubstituted thiocarbamoylthio) pyrazoles and two thiocyanatopyrazoles were synthesized. Antifungal activities of these compounds as well as those described in the preceding paper were tested. In conclusion, 4-thiocyanatopyrazoles showed high antifungal activities of which 1-(m-nitrophenyl)-4-thiocyanato-3, 5-dimethylpyrazole was most effective.View full abstractDownload PDF (728K) -
Tadashi Sasaki, Ken Kanematsu, Katsumaro Minamoto, Hajime Fujimura1964 Volume 12 Issue 2 Pages 191-195
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1) 2-Dialkylamino-2-phenylacetophenone was prepared. 2) The Mannich reaction of deoxybenzoin was described. 3) The compounds of VI and IX were found to possess less toxic and more analgesic properties than (±) N, N-dimethyl-1, 2-diphenylethylethylamine.View full abstractDownload PDF (543K) -
Hidehiko Kaneko, Masahisa Hashimoto, Akio Kobayashi1964 Volume 12 Issue 2 Pages 196-203
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Dimethylaminomethylestrone (Ia) and the 4-isomer (IIa) were obtained from the Mannich product of estrone. Methiodides of I'a-c and II'a-c were treated with alcoholic alkali to give 2-and 4-alkoxymethylestrogens in good yields. Methylation in the usual manner of I and II failed, but reaction of I and II with dimethylsulfate in a boiling methanolic alkali gave the 3-methyl ethers of 2-and 4-methoxymethylestrogens, respectively. The structural assignments of the isomers were discussed based on nuclear magnetic resonance, infrared and ultraviolet spectra.View full abstractDownload PDF (926K) -
Yasuo Makisumi, Haruyuki Watanabe, Kazuo Tori1964 Volume 12 Issue 2 Pages 204-212
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSProton magnetic resonance spectra of the s-triazolo [1, 5-α] pyrimidine derivatives are recorded to give the positional order of H6>H2>H5>H7 for the ring proton chemical shifts in τ-value. The methyl substituent effect on the proton chemical shifts and the correlation between the proton chemical shift and the local π-electron density on the carbon atom to which the proton is bonded, are discussed. Thus the charge densities determined from proton chemical shifts show a remarkably good correspondence with the charge distributions calculated by the simple Huckel MO method.View full abstractDownload PDF (1018K) -
Shin-ichi Ueda1964 Volume 12 Issue 2 Pages 212-214
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDibenzo-p-dioxin-2, 7-dicarboxylic acid (III) in concentrated sulfuric acid with potassium nitrate gave an electron spin resonance spectrum which was considerably similar to that of dibenzo-p-dioxin-2, 7-disulfonic acid (II). Therefore, the spectra indicated that the distributions of the spin densities of the odd electron were quite similar in both cases.View full abstractDownload PDF (391K) -
Tadasu Tanaka1964 Volume 12 Issue 2 Pages 214-223
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-(o-Methoxymethoxybenzoyl)-1, 3-cyclohexanedione, having a β-tricarbonyl system, was synthesized by the interaction of disodio-1, 3-cyclohexanediene and methyl o-methoxymethoxybenzoate in liquid ammonia. 4-(o-Hydroxybenzoyl)-1, 3-cyclohexanedione, having a hypothetical β-tetracarbonyl system, was also prepared. Grisan-2', 3, 4'-trione yielded from the β-tetraketone by means of alkaline ferricyanide oxidation. The structures of its two isomeric methyl enol ethers were proved by deriving them to grisan-2', 3-and grisan-3, 4'-dione.View full abstractDownload PDF (1062K) -
Makoto Hayashi, Reiko Uchida, Tsutomu Unemoto, Komei Miyaki1964 Volume 12 Issue 2 Pages 223-227
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn enzyme oxidizing ethanolamine was partially purified from beef serum by fractionation with ammonium sulfate and DEAE-cellulose column chromatography. This partially purified preparation showed an optimum pH of 7.5 and apparent Km of 4×10-3M for ethanolamine. Without regard to the addition of catalase, the ratio of oxygen consumption to ammonia formation was 1 : 1 and the oxidation product of ethanolamine was identified as glyoxal.View full abstractDownload PDF (599K) -
Potential Anticancer agents. XIV. Reaction of 3-Substituted Pyridazine 1-Oxide with Benzoyl Nitrate.Takanobu Itai, Sachiko Natsume1964 Volume 12 Issue 2 Pages 228-235
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe nitration of 3-methyl-, 3, 6-dimethyl-, and 3-methoxypyridazine 1-oxide with benzoyl chloride-silver nitrate afforded their corresponding 5-nitro derivatives, while in the reaction of 3, 6-dimethoxypyridazine 1-oxide with the same reagents, no nitro compound was detected but 1-hydroxy-3-methoxy-6 (1H)-pyridazinone and its benzoyl derivative were produced. Some nucleophilic substitution reactions related to 5-nitropyridazine 1-oxides obtained here, were described.View full abstractDownload PDF (875K) -
Shinsaku Natori, Hidejiro Nishikawa, Hideko Ogawa1964 Volume 12 Issue 2 Pages 236-243
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of helicobasidin, a major pigment of Helicobasidium mompa TANAKA, was proved to be (S)-3-methyl-2, 5-dihydroxy-6-(1, 2, 2-trimethylcyclopentyl) benzoquinone (IV).View full abstractDownload PDF (774K) -
Shumichi Yamada, AbdulMohsen Omar, Tohru Hino1964 Volume 12 Issue 2 Pages 244-249
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeveral N-(2-arylethyl)-substituted thioamides (IVa∼IVf) were synthesized from the dithioesters (V or VI) and the 2-arylethylamines in good yield, in order to test direct cyclization of the thioamides to the corresponding 3, 4-dihydroisoquinolines by a Bischler-Napieralski type reaction The comparative study of the infrared absorption spectra of the thioamides with those of the corresponding acid amides shows that the most characteristic absorption bands of the C=S group in the thioamides (IVa∼IVf) fall within four regions, namely, 1508∼1520, 1388∼1416, 1330∼1352, and 1100∼1150cm-1.View full abstractDownload PDF (655K) -
Shunichi Yamada, AbdulMohsen Omar1964 Volume 12 Issue 2 Pages 249-252
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThioamides have been cyclized in good yield to the corresponding 1-substituted 3, 4-dihydroisoquinoline under the normal Bischler-Napieralski reaction conditions which are generally used to cyclize acid amides. Phosphorus pentasulfide has been effectively used as a condensing agent in the Bischler-Napieralski reaction to get 1-substituted-3, 4-dihydroquinoline from both thioamides as well as normal acid amides.View full abstractDownload PDF (615K) -
Hiroyuki Inouye, Toshio Arai, Yoshihito Yaoi, Muneharu Ogawa1964 Volume 12 Issue 2 Pages 255-256
Published: February 25, 1964
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (356K)
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