1 0 0 0 OA Syntheses of 2-(3, 4-Dimethoxyphenyl)ethylamine Derivatives and Their Antiulcer Activities
- 著者
- 細上 徹 榑谷 昌彦 東 邦彦 浅野 昌英 大屋 和美 高杉 紀雄 真船 英一 三木 藤作
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.40, no.10, pp.2712-2719, 1992-10-25 (Released:2008-03-31)
- 参考文献数
- 18
- 被引用文献数
- 12 14
A series of acyl derivatives of 2-(3, 4-dimethoxyphenyl)ethylamine (4) were synthesized and evaluated for their effectiveness to prevent water-immersion stress-induced gastric ulceration when given intraperitoneally to rats. Among them N-[2-(3, 4-dimethoxyphenyl)ethyl]-2-phenylaminoacetamide hydrochloride (15) had significant antiulcer activity. Further modification of the four parts of 15 revealed that only the introduction of a carbamoyl group into 2- or 3-position of the phenylamino part gave compounds (49-51, 54 and 55) which retained antiulcer activity comparable to the lead compound. However, the compounds (49-51 and 54) did not exert a prophylactic effect when administered orally except for the 3-substituted bezamide derivative 55. Alkyl substitution on the nitrogen of benzamide gave 3-[[[2-(3, 4-dimethoxyphenyl)ethyl]carbamoyl]methyl]amino-N-methylbenzamide (66, DQ-2511) and the related compounds (67, 70, 74 and 77) which all had potent antiuler activities at oral doses of 50-400 mg/kg.
1 0 0 0 OA Thermal Dehydration of Nafagrel Hydrochloride Hydrate at Controlled Water Vapor Partial Pressures
- 著者
- 北岡 宏章 大屋 和美 伯水 英夫
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.43, no.10, pp.1744-1750, 1995-10-15 (Released:2008-03-31)
- 参考文献数
- 11
- 被引用文献数
- 6 6
Nafagrel hydrochloride exists as both a hemihydrate and monohydrate. Conversion from the hemihydrate to the monohydrate is not reversible, and both hydrates can coexist in stable equilibrium between 23% relative humidity (RH) and 64% RH. In order to clarify the dehydration behavior, the kinetics of the thermal dehydration of the hydrates was studied by means of isothermal gravimetry at atmospheric pressure with a controlled water vapor pressure. This revealed that dehydration did not depend on absolute humidity but on RH. The dehydration of the hemihydrate proceeded by two-dimensional gorwth of the nuclei, A2, but the mechanism of monohydrate dehydration changed from A2 to a two-dimensional phase boundary, R2, with an increase in RH. The dehydration of the monohydrate proceeded by R2, resulting in the production of the hemihydrate at 6.5% RH or above. These kinetic analyses showed that the monohydrate dehydrated faster than the hemihydrate.