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Synthesis and analgesic activity of hydrochlorides and quaternary ammoniums of epibatidine incorporated with amino acid ester
Dong, JC; Wang, X; Li, RT; Zhang, HM; Cheng, TM; Li, CL
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2003-12-15
DOI10.1016/j.bmcl.2003.09.047
13期:24页:4327-4329
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]NICOTINIC ACETYLCHOLINE-RECEPTORS ; UNIQUE SPIROCYCLOPIPERAZINIUM SALT ; POISON FROG ; ANALOGS ; (+/-)-EPIBATIDINE ; AGONIST ; BINDING ; LIGAND ; BRAIN
英文摘要

Hydrochloride derivatives 5a-c and quaternary ammonium derivatives 6a-c of epibatidine incorporated with amino acid ester were synthesized and evaluated for their in vivo analgesic activity and toxicity. Among all tested compounds, compound 6c has the most potent analgesic activity. The quaternary ammonium salts 6a and 6c showed better analgesic activity than the corresponding hydrochlorides 5a and 5c. Both 5a-c and 6a-c showed significantly lower toxicity than epibatidine itself. (C) 2003 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000187010700014
引用统计
被引频次:7[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/400002259/62181
专题北京大学药学院
作者单位Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Dong, JC,Wang, X,Li, RT,et al. Synthesis and analgesic activity of hydrochlorides and quaternary ammoniums of epibatidine incorporated with amino acid ester[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2003,13(24):4327-4329.
APA Dong, JC,Wang, X,Li, RT,Zhang, HM,Cheng, TM,&Li, CL.(2003).Synthesis and analgesic activity of hydrochlorides and quaternary ammoniums of epibatidine incorporated with amino acid ester.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,13(24),4327-4329.
MLA Dong, JC,et al."Synthesis and analgesic activity of hydrochlorides and quaternary ammoniums of epibatidine incorporated with amino acid ester".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 13.24(2003):4327-4329.
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