The pharmacological factors which affect the stress ulcer formation were studied in rats Some gastric functions, mainly gastric motility, secretion, blood circulation and protective action of gastric mucosa play the important roles in the ulcer formation induced by the stress which was inflicted by immobilization and immersing in water. Effect of some pharmacedynamic agents on the stress ulcer was examined, and it was found that the secretagogue action is more important than the other pharmacodynamic action tested. Effects of anticholinergics on the gastric functions were also studied, and the close relations between antiulcerous effect and depressive activity of gastric secretion and motility was confirmed. The protective action of gastric mucosa against gastric juice was estimated and the effect of stress and atropine on it was examined. Atropine seemed to have the effect inhibiting the decrease of the protective action of gastric mucosa.

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Hydrogen ion liberation from AET and APT was investigated. In the presence of alkali less approximately one equivalent with respect to aminoalkylisothiuronium salt, hydrogen ion liberation was observed. In the presence of alkali more than one equivalent, hydrogen ion liberation was not occured. This reaction was attributed to the intramolecular transguanylation which was accompanied with the acid dissociation of AET and APT. The rate of hydrogen ion liberation was more than twenty times fast in AET. The ratio of activation energy was 20 or 30 per cent larger in AET than in APT. In the absence of alkali, AET was transformed to 2-aminothiazoline and ammonium ion was splitted off. While the cyclization of APT was scarcely observed in the same condition.

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Stability constants, log K₁ and log K₂, of complexes of D-glucosaminic acid with Cu²⁺, Ni²⁺, Pb²⁺, Zn²⁺, Co²⁺, Cd²⁺, and Mn²⁺were determined by pH titration method. Copper complexes were found to be the most stable and the contribution of OH groups of glucosaminic acid to the complex formation was observed.

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Gas chromatography of copper (II) and nickel (II) chelates of β-ketoimine type derivatives of 2, 4-pentanedione and salicylaldehyde were investigated. Copper and nickel chelates of 4-imino-2-pentanone gave definite peaks and their separation was attained. Furthermore, the determination of nickel chelate of 4-imino-2-pentanone was investigated.

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Potassium 2-methyl-5-hydroxy-6, 7-benzochromon-8-y1 sulfate (VIII) and potassium 2-methyl-5-hydroxy-7, 8-benzochromon-6-y1 sulfate (IX) were synthesized from 2-methyl-5, 8-dihydroxy-6, 7-benzochromone (I) and 2-methyl-5, 6-dihydroxy-7, 8-benzochromone (II). Hydroxylation of 2-methyl-5-hydroxy-6, 7-benzochromone (III) and 2-methyl-5-hydroxy-7, 8-benzochromone (IV) gave 2-methyl-4H-naphtho[2, 3-b]pyran-4, 5, 10(5H, 10H)-trione (V) from both, and the mechanisms of the abnormal reaction were investigated. It was found that V is also obtained from IX in the same condition as hydroxylation and that 2-methyl-4H-naphtho[1, 2-b]pyran-4, 5, 6(5H, 6H)-trione (X) underwent ring isomerization to V directly or through a diketone, 2-acetoacetyl-3-hydroxy-1, 4-naphthoquinone (XI), as an intermadiate. Synthesis of I from II and that of 2-methyl-3-acetyl-5, 8-dihydroxy-6, 7-benzochromone (VI) from 2-methyl-3-acethyl-5, 6-dihydroxy-7, 8-benzochromone (VII) was accomplished by the application of a novel reaction together with a new oxidation method using sodium nitrite. VI also underwent ring isomerization to VII. Thus, it was found that acetyl group at 3-position in VI or 2-methyl-3-acetyl-4H-naphtho[1, 2-b]pyran-4, 5, 6(5H, 6H)-trione (XIII) was not eliminated during two kinds of ring isomerization described.

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Syntheses of hydroxyl derivatives of 2-methyl-5, 6-bezochromone were investigated, and following benzochromone derivatives were obtained together with related compounds, and physical and chemical properties of these chromones were characterized : 2-Methyl-8-methoxy-5, 6-benzochromone (IV), 2-methyl-7-methoxy-5, 6-benzochromone (X), 2-methyl-7, 8-dimethoxy-5, 6-benzochromone (XIV), 2-methyl-3-acetyl-8-methoxy-5, 6-benzochromone (XXV), 2-methyl-3-acetyl-7-methoxy-5, 6-benzochromone (XXII), and 2-methyl-3-acetyl-7, 8-dimethoxy-5, 6-benzochromone (XXIII). Hydroxylation of 2-methyl-8-hydroxy-5, 6-benzochromone (III) or 2-methyl-7-hydroxy-5, 6-benzochromone (V) gave 2-methyl-7, 8-dihydroxy-5, 6-benzochromone (XX) from both.

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Seventy-one possible sulfhydryl reagents were examined on the chemical reactivity with methyl N-acetylcysteinate, as well as on the inactivating ability against adenovirus type 5. It has been found that the compounds capable of inactivating the virus are always accompanied by the chemical reactivity with the SH group of methyl N-acetylcysteinate, and that the compounds incapable of reacting with the SH group are unable to exhibit the virus-inactivating activity either. Above all, the compounds, whose chlorine atom is directly linked to a nitrogen atom, have shown a marked virus inactivating activity.

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As the starting material for the synthesis of sparteine derivatives, 5-oxosparteine (II) was synthesized. Condensation of Δ⁵-dehydrosparteine (IX) or Δ¹⁽⁶⁾-dehydrosparteinium ion (VIII) and benzaldehyde gave 5-benzylidene-Δ¹⁽⁶⁾-dehydrosparteinium ion (X) which was reduced to 5-benzylidenespartein (XI), and its oxidative cleave should have provied II but the objective was not attained. 5-Hydroximinosparteinium ion was obtained by the condensation of IX and nitrosyl chloride or VIII and ethyl nitrite, this sparteinium ion was reduced to 5-hydroximinosparteine (XIII), and its treatment with pyruvic acid gave the objective II. II has the same configuration as that of sparteine.

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1. The penetrating rate constants of water and ethanol into magnesium oxide and AS powder beds were obtained with a satisfactory reproducibility. These results were in accord with Washburn's equation. 2. The penetrating rate constants in these systems were dependent on the temperature of liquid according to log k/T=α-β/RT and apparent activation energies of wetting were obtained as a few kcal. 3. Dependence of the penetrating rate constant on moisture content of powder was remarkable in systems of relatively small k values like AS/water and magnesium oxide/ethanol. 4. The apparent activation energy of wetting was concerned with the moisture content of powder. 5. The disintegration time of tablet was dependent on the temperature of liquid as well as on the compressional force. The temperature dependence of disintegration time was almost the same as that of penetrating rate constant. 6. The immersional wetting might be a controlling factor on the disintefration of the tablet made under a low compressional force.

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Commercial DAHG J.P. (G-A and G-B) were kept in various atmosphere under relative humidity and in distilled water at 30° and the following results were obtained. 1. BET specific surface area by the adsorption of water was a little larger than that by the adsorption of nitrogen and the difference between both values of G-B, which had less specific surface area and inferior anti-aging properties, was larger. 2. When both samples were kept standing under high humidity or in water, at an early stage of the aging process, their neutralizing rates became faster temporarily. This phenomenon was observed remarkably with G-B. 3. The sample aged under high humidity with the lapse of time were considered to change in the following process : Amorphous→boehmite-like substance→bayerite + gibbsite ; i.e., finally transferred to a mixture of bayerite and gibbsite. 4. Infrared absorption spectra of the aged samples, which lost the neutralizing reactivity, showed their characteristic absorption band around 1020∼960 cm^-1.

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The intestinal absorption of sulfisoxazole was reduced by replacing sodium ion in perfusion solution with potassium ion in vivo. The rates of intestinal transport of sulfonamide, sulfisoxazole and sulfisomezole, also, were decreased by replacing sodium ion in circulating solution with potassium ion in vitro. The transport rate and uptake of sulfisomezole in the intestine were decreased by DNP alone, and the combination of the replacing sodium ion with potassium ion and DNP. These of sulfisoxazole and sulfanilamide, however, were not affected by the same treatments.

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A variety of the steroidal 17-oximes and their O-alkyl, especially O-(2-dimethyl-aminoethyl) derivatives are prepared from the corresponding 17-ketones. A marked anesthetic, hypocholesterolemic and/or antifungal activities of some of these compounds are described.

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2-Subsituted 3-diphenylmethylene-1-pyrrolines (III) were synthesized in one step by the reaction of 1, 1-diphenyl-1, 4-butanediol (VII), 2, 2-diphenyltetrahydrofuran (VI), or 4-bromo-1, 1-diphenyl-1-butene (V) with nitrile-stannic chloride complex. 2, 5-Dimethyl (XI) and 2, 5, 5-trimethyl-3-diphenylmethylene-1-pyrroline (XII) were obtained respectively from 1, 1-diphenyl-1, 4-pentanediol (IX) and 1, 1-diphenyl-4-methyl-1, 4-pentanediol (X). The fact that 2-methyl-3-isopropylidene-1-pyrroline (XIV) was obtained from 2-methyl-2, 5-pentanediol (XIII) and 2, 2-dimethyltetrahydrofuran (XV) by the same reaction was of interest in contrast with preparation of 1-pyrrolines (II) by the Ritter reaction. Reduction of the methiodide of III with sodium borohydride gave 1-methyl-2-alkyl-3-diphenylmethylenepyrrolidine. The methiodide of the 2-methyl compound (XVIc) was found to have a comparatively strong anti-acetylcholine activity.

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