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学科主题: 药学
题名:
N-[2-(5,5-Dimethyl-1,3-dioxane-2-yl)ethyl]amino acids: Their synthesis, anti-inflammatory evaluation and QSAR analysis
作者: Li, Xiangmin2; Zhao, Ming3; Tang, Yu-Rong1; Wang, Chao2; Zhang, Ziding1; Peng, Shiqi3
关键词: anti-inflammatory drug ; chemical synthesis ; amino acid ; 1,3-dioxane ; QSAR
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2008
DOI: 10.1016/j.ejmech.2007.03.015
卷: 43, 期:1, 页:8-18
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: INFRARED-SPECTRA ; 3D STRUCTURE ; INFLAMMATION ; CANCER
英文摘要:

Developing novel anti-inflammatory drugs is increasingly important in modern pharmaceutical industry. In this work, the reactions of both amino acids and their methylesters with 3-(5,5-dimethyl-1,3-dioxane-2-yl)propanal (2) were performed to either directly provide the goal products N-[2-(5,5-dimethyl-1,3-dioxane-2-yl)ethyl]amino acids (4a-s) in 9-65% yields or provide the intermediates N-[2-(5,5-dimethyl-1.3-dioxane-2-yl)ethyl]amino acid methylesters (3a-s) in 78-87% yields. The saponification of 3a-s provided 4a-s in 80-89% yields. Using a xylene-induced ear edema model, the anti-inflammatory activities of these newly synthesized anti-inflammatory agents were evaluated. The results indicated that comparing to the vehicle control 17 out of 4a-s significantly inhibited the development of inflammation in mice (p < 0.01). In particular, eight out of 4a-s exhibited an even higher anti-inflammatory activity than the standard reference drug aspirin (p < 0.05-0.01). A QSAR analysis was performed by use of the molecular descriptors generated from e-dragon software. The predictive accuracy of the established QSAR model implies that it may be promising for screening the new derivatives of 2-position amino acid substituted 1,3-dioxanes as potential anti-inflammatory agents. (C) 2007 Elsevier Masson SAS. All rights reserved.

语种: 英语
WOS记录号: WOS:000253274300002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66899
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.China Agr Univ, Coll Biol Sci, Beijing 100094, Peoples R China
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
3.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100054, Peoples R China

Recommended Citation:
Li, Xiangmin,Zhao, Ming,Tang, Yu-Rong,et al. N-[2-(5,5-Dimethyl-1,3-dioxane-2-yl)ethyl]amino acids: Their synthesis, anti-inflammatory evaluation and QSAR analysis[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2008,43(1):8-18.
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