IR@PKUHSC  > 北京大学药学院
学科主题药学
Novel 1-oxyl-2-substitutedphenyl-4,4,5,5-tetramethylimidazolines: Synthesis, selectively analgesic action, and QSAR analysis
Zhao, Ming; Li, Zheng; Peng, Li; Tang, Yu-Rong; Wang, Chao; Zhang, Ziding; Peng, Shiqi
关键词tetramethylimidazoline analgesic vasorelaxation QSAR
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2007-04-15
DOI10.1016/j.bmc.2007.02.023
15期:8页:2815-2826
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]ADRENERGIC-RECEPTORS ; ANTAGONISTS ; POTENT ; IMIDAZOLINES ; DERIVATIVES ; AGONISTS ; ANALOGS ; RATS ; MICE ; SAR
英文摘要

Based on the knowledge that imidazoline can result in analgesic action due to its selective binding with the prostacyclin receptor, 20 1-oxyl-2-substitutedphenyl-4,4,5,5-tetramethylimidazolines (3a-t) were prepared in moderate yields. At 0.13 mmol/kg dose, their in vivo analgesic activities were evaluated after the mice were administered at 30, 60, 90, and 150 min. Compared with the pain threshold (12.27 +/- 9.56-17.71 +/- 7.00%) of normal saline (NS) receiving mice, the pain threshold (23.42 +/- 8.14% to 102.58 +/- 10.66%) of 3a-t receiving mice increases significantly. Considering a prostacyclin receptor targeting analgesic agent usually had bleeding action and to appraise the bleeding risk, the in vivo tail bleeding time of 1.30 mmol/kg 3a-t receiving mice was found to be ranged from 116.3 +/- 8.2 s to 120.3 +/- 9.2 s, which was substantially equal to that (117.8 +/- 8.4 s to 119.0 +/- 8.6 s) of NS receiving mice. Based on the possibility of imidazoline acting as vasodilator, the in vitro vasorelaxations of 3a-t were tested using the rat aortic strip model. When the aortic strip contracted by noradrenaline (NE, final concentration 10(-7) mol/l) was treated with 3a-t (final concentration 5 x 10(-4) mol/l), only lower percentage inhibitions (6.55 +/- 5.70-37.40 +/- 4.07%) were recorded, implying that the vasorelaxation of 3a-t was neglectable. By selecting appropriate molecular descriptors generated from e-dragon server, the QSAR model of the analgesic activities of 3a-t was constructed using the multiple linear regression method. The established QSAR model showed reasonable accuracy and thus it is promising to be used for screening new 1-oxyl-2-substitutedphenyl-4,4,5,5-tetramethylimidazoline derivatives as analgesic agents. (c) 2007 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000245637200002
引用统计
被引频次:6[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/68178
专题北京大学药学院
作者单位1.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100054, Peoples R China
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
3.China Agr Univ, Coll Biol Sci, Beijing 100094, Peoples R China
推荐引用方式
GB/T 7714
Zhao, Ming,Li, Zheng,Peng, Li,et al. Novel 1-oxyl-2-substitutedphenyl-4,4,5,5-tetramethylimidazolines: Synthesis, selectively analgesic action, and QSAR analysis[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(8):2815-2826.
APA Zhao, Ming.,Li, Zheng.,Peng, Li.,Tang, Yu-Rong.,Wang, Chao.,...&Peng, Shiqi.(2007).Novel 1-oxyl-2-substitutedphenyl-4,4,5,5-tetramethylimidazolines: Synthesis, selectively analgesic action, and QSAR analysis.BIOORGANIC & MEDICINAL CHEMISTRY,15(8),2815-2826.
MLA Zhao, Ming,et al."Novel 1-oxyl-2-substitutedphenyl-4,4,5,5-tetramethylimidazolines: Synthesis, selectively analgesic action, and QSAR analysis".BIOORGANIC & MEDICINAL CHEMISTRY 15.8(2007):2815-2826.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Zhao, Ming]的文章
[Li, Zheng]的文章
[Peng, Li]的文章
百度学术
百度学术中相似的文章
[Zhao, Ming]的文章
[Li, Zheng]的文章
[Peng, Li]的文章
必应学术
必应学术中相似的文章
[Zhao, Ming]的文章
[Li, Zheng]的文章
[Peng, Li]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。