YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
84 巻 , 3 号
選択された号の論文の20件中1~20を表示しています
  • ニトロフラン核を有する2-Alkylthiopyrimidine類の合成および構造活性相関について
    才川 勇
    1964 年 84 巻 3 号 p. 207-212
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    2-Alkylthio-4-(5-nitro-2-furylalkenyl)pyrimidines (VI) shown in Table I were readily obtained by an acid-catalyzed condensation of 2-alkylthio-4-methylpyrimidines (IV) with 5-nitro-2-furyl-aldehydes (V) in a fairly good yield. VI was highly susceptible to photodecomposition and some of them failed to show normal ultraviolet absorption spectra. Antibacterial activity of VI against Escherichia coli O-18 and Staphylococcus aureus 209P was tested in three kinds of bouillon medium, and the result (Table III) showed that 2-methylthio-4-[3-methyl-4-(5-nitro-2-furyl)-1, 3-butadienyl]pyrimidine had the highest activity among them.
  • ニトロフラン核を有する2-Amino-1,3,4-oxadiazole系化合物の合成ならびに構造活性相関について
    才川 勇
    1964 年 84 巻 3 号 p. 212-219
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    2-Amino-5-(5-nitro-2-furylalkenyl)-1, 3, 4-oxadiazoles (IV) were prepared by the known methods and their antibacterial activity was tested.
    IV was less effective than 3-amino-6-(5-nitro-2-furylalkenyl)-1, 2, 4-triazines (II), but their structure-activity relationship was quite similar to that of II. IV (R1=H, n=0) was reacted with excess formaldehyde and 2-[bis(hydroxymethyl)amino]-5-[2-(5-nitro-2-furyl)vinyl]-1, 3, 4-oxadiazole (XVI) was obtained.
    The protective effect of XVI in mice was tested and it was found to have stronger in vivo activity than 3-[bis(hydroxymethyl)amino]-6-[2-(5-nitro-2-furyl)vinyl]-1, 2, 4-triazine (I).
  • ニトロフラン核を有する2-(Substituted amino)-1,3,4-oxadiazole系化合物の合成ならびに構造活性相関について
    才川 勇, 高井 明, 見玉 寛
    1964 年 84 巻 3 号 p. 219-224
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    2-(Monosubstituted amino)-5-(5-nitro-2-furylalkenyl)-1, 3, 4-oxadiazoles (V) were prepared and their antibacterial activity was tested. Among them, the protective effect of 2-methylamino-5-[2-(5-nitro-2-furyl)vinyl]-1, 3, 4-oxadiazole (V:R1=H, n=0, R3=CH3) was tested in mice and it was found to have the same in vivo activity spectrum as 2-[bis(hydroxymethyl)amino]-5-[2-(5-nitro-2-furyl)vinyl]-1, 3, 4-oxadiazole.
  • ニトロフラン核を有する1,3,4-Oxadiazole系化合物の合成ならびに構造活性相関について
    才川 勇, 高井 明, 児玉 寛
    1964 年 84 巻 3 号 p. 225-229
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    2-Substituted 5-[2-(5-nitro-2-furyl)vinyl]-1, 3, 4-oxadiazoles (I), in which H, OH, SH, SCH3, alkyl, or phenyl radical was substituted at 2-position in the oxadiazole ring, were prepared by the known methods and their antibacterial activity was tested, but none was so effective as 2-(amino-substituted)-1, 3, 4-oxadiazole derivatives in vivo test.
  • 林 平三郎, 見奈美 秀蔵
    1964 年 84 巻 3 号 p. 229-236
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    Examinations were made on the quantitative relationship between the repose angle, a flow property of powders measured by the tilting-box method, and various primary factors connected with that repose angle such as the length of powder tilting surface, interparticle cohesion, coefficient of internal friction, and apparent density of the powder.
    1) The repose angle i increased with decreasing the length of tilted surface, i.e., the length of the tilting box, L.
    2) If the values of the coefficient of internal friction and apparent density γ are not exceedingly different between two kinds of powders, fluidity of the powder expressed by the repose angle is closely correlated to the interparticle cohesion (c).
    3) When the apparent density is small, that powder has a poor fluidity.
    These relationships found by experiments were found to agree well with the general formula for the repose angle, 2c⋅cosφ/γL=sin2{(i-φ)/2}, (where φ is the angle of internal friction) derived kinetically from the equilibrium conditions of the force acting on tilted powder surface. Using this formula, the value of c was calculated and the value was compared with that measured by the shear test.
  • 種々のカルビノールおよびフェノール類のメタンスルホネートの合成ならびにその生物学的活性
    亀谷 哲治, 梅沢 修, 関根 清子, 織田 健, 石黒 正子, 水野 伝一
    1964 年 84 巻 3 号 p. 237-246
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    There have been numerous reports on Myleran among various alkyl methanesulfonates and 39 kinds of various derivatives of carbinols were synthesized to examine their antibacterial, antifungal, and antitumor actions. A large number of methanesulfonates of various phenolic compounds were synthesized and their antitumor action was examined. Among these compounds, 2-chloro-3′, 4′-dimethoxyacetophene was found to have considerable effect against Ehrlich ascites tumor.
    Reaction of pyrocatechol with chloroacetyl chloride and chloropropionyl chloride was also examined.
  • 電解質およびアニオン性界面活性剤の電気伝導度について
    中垣 正幸, 河村 成男
    1964 年 84 巻 3 号 p. 246-251
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    Electrical conductivity of sodium chloride, potassium chloride, and sodium lauryl sulfate in 0, 3, 10, 20, and 30% aqueous sucrose solutions was measured in concentration between 0.0002 and 0.04M. The apparent radius of Na+, K+, and Cl- was calculated from the limiting equivalent conductivity Λ of sodium and potassium chloride in aqueous sucrose solutions on the basis of Stokes' law. The apparent radius of these ions decreased linearly with increasing sucrose concentration. This is considered to be due to the partial dehydration of ions by the addition of sucrose.
    The equivalent conductivity Λ of sodium chloride, potassium chloride, and sodium lauryl sulfate decreased by the increase of sucrose concentration. The decrease of mobility of ions is considered to be due mainly to the increase of viscosity of the medium by the addition of sucrose. Λη0-√c curves, however, showed that Λη0 increased with sucrose concentration. This phenomenon seems to be due to the decrease of the radius of ions through dehydration by sucrose.
    The critical micelle concentration of sodium lauryl sulfate decreased by the increase of sucrose concentration. This phenomenon is also considered to be due to dehydration by sucrose.
  • 小島 操, 仲道 述夫, 塩谷 桂子
    1964 年 84 巻 3 号 p. 251-255
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    Reaction of allyl isothiocyanate with sugar reagents was examined and the compound was found to react with all reagents based on reducibility. Sugar reagents using copper sulfate produced a black precipitate which is probably due to the formation of copper (II) sulfide besides copper (I) oxide.
    Allyl isothiocyanate can be quantitatively determined by the Bertrand method and is also possible by the 3, 5-dinitrosalicylic acid method if care is taken with reaction conditions (90±2°, heated for 30 min.).
    Reduction of sugar reagents by allyl isothiocyanate is due to the reducibility of sodium sulfide which is formed on being heated with sodium hydroxide.
  • 数種のノルモルヒネおよび14-ヒドロキシノルモルヒノン誘導体の薬理作用
    関 功, 高木 弘, 小林 晋作
    1964 年 84 巻 3 号 p. 255-267
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    The compounds having morphine rings on both ends of 2-butyne, 1, 4-bis(normorphino)-2-butyne dimethiodide (I), 1, 4-bis(norcodeino)-2-butyne dimethiodide (II), and 1, 4-bis(14-hydroxydihydronorcodeinono)-2-butyne dihydrochloride (III), did not show strong analgesic action or antagonism against morphine. Of these three compounds, III showed anti-barium action close to that of papaverine. Both N-allyl and N-propargyl compounds showed antagonism against morphine and this action was stronger in the former. Antagonism against morphine was seen in any of the actions such as analgesism, suppression of avoidance reactions, hypotension, respiration inhibition, and slowing of brain wave. Toxicity was the weakest in N-propargyl compound. The antagonistic action of N-propargyl-14-dihydroxydihydronormorphinone (RAM-302) against morphine was comparable to that of nalorphine and its toxicity was lower. This antagonistic action against morphine was the same as in the case of analgesic action and the 3-hydroxy compound had stronger action than the 3-methoxy compound.
  • 数種の14-ヒドロキシ-6-デオキシモルヒネ系化合物の薬理作用
    関 功, 高木 弘, 小林 晋作, 出口 健彦, 熊倉 清治
    1964 年 84 巻 3 号 p. 268-279
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    Physiological action of 14-hydroxy-6-deoxy morphine derivatives was examined; analgesic action, suppression of avoidance reactions, fortification of thiopental anesthesia, action on brain wave of rabbit cerebral cortex, actions on blood pressure and respiration, and action on excised intestine. N-Phenethyl-14-hydroxydeoxydihydronormorphine (RAM-315) has analgesic action 70 times that of morphine, as well as stronger actions in other points. The N-methyl compound (RAM-307) shows 10 times stronger action than morphine. In general, 6-deoxy compounds have stronger action and stronger toxicity. N-Allyl and N-propargyl compounds show antagonism against morphine, that of N-allyl-14-hydroxydeoxydihydronormorphine (RAM-313) being five times that of nalorphine.
  • 14-ヒドロキシモルヒネ誘導体の化学構造と作用との関係について
    関 功, 高木 弘, 小林 晋作
    1964 年 84 巻 3 号 p. 280-286
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    About 80 kinds of new derivatives of morphine possessing a hydroxyl in 14-position were synthesized and the effect of this introduction of hydroxyl on acute toxicity, analgesic action, and antitussive action was examined. in general, the introduction of hydroxyl resulted in reduction of toxicity and increased analgesic and antitussive actions. In N-substituted compounds, N-phenethyl compound had stronger toxicity than the N-methyl compound, and analgesic action was also stronger. N-Pentyl, N-phenacyl, and non-substituted compounds had weak actions. Etherification of the hydroxyl in 3-position resulted in decreased analgesic and antitussive actions. Etherification of hydroxyl in 4-position of morphinan derivatives results in fortification of toxicity, analgesic and antitussive actions, the action being marked in methyl ethers. Both the analgesic and antitussive actions, and toxicity become stronger in 6-oxo and 6-deoxy compounds than in 6-hydroxy compounds. These tendencies are approximately the same as those of compounds not possessing a hydroxyl in 14-position.
  • α-Picoline N-Oxideとα-Haloketoneとの反応
    加藤 鉄三, 後藤 良宣, 山本 豊
    1964 年 84 巻 3 号 p. 287-289
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    When α-picoline 1-oxide and phenacyl bromide are mixed under cooling and the solidified crystals are washed with anhydrous ether and benzene, O-phenacyl compound (I), m.p. 70°, of α-picoline 1-oxide is obtained. Basification of this product (I) with sodium carbonate gives phenylglyoxal easily in ca. 50% yield. If a solvent is used and the mixture is heated, this yield becomes lower. The use of acetone produces α-picoline 1-oxide 1/2hydrobromide (II), m.p. 142°. Reaction of α-picoline 1-oxide and α-bromoacetone in benzene gave pyruvic aldehyde in 26% yield.
  • 加藤 鉄三, 後藤 良宣, 近藤 正嗣
    1964 年 84 巻 3 号 p. 290-292
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
    Quinaldine 1-oxide reacts with amyl nitrite in liquid ammonia, in the presence of metal amide, and produces quinaldaldehyde 1-oxide oxime (II) in 27-51% yield, with by-product formation of quinaldonitrile 1-oxide (III), quinaldamide 1-oxide (IV), qninaldonitrile (V), and quinaldamide.
    The same reaction of lepidine 1-oxide resulted in the difficulty of separating the product but formation of cinchoninaldehyde 1-oxide oxime was proved by its isolation.
    Quinaldine and lepidine both easily afforded the corresponding quinolinecarboxaldehyde oxime in a good yield of 55-67%.
  • 薬学研究長期計画委員会
    1964 年 84 巻 3 号 p. APreface1
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
  • 1964 年 84 巻 3 号 p. A1-A4
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
  • 1964 年 84 巻 3 号 p. A5-A18
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
  • 1964 年 84 巻 3 号 p. A19-A32
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
  • 1964 年 84 巻 3 号 p. A33-A44
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
  • 1964 年 84 巻 3 号 p. A45-A55
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
  • 1964 年 84 巻 3 号 p. A56-A58
    発行日: 1964/03/25
    公開日: 2010/02/19
    ジャーナル フリー
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