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学科主题: 药学
题名:
Unique spirocyclopiperazinium salt. Part 2: Synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics
作者: Wang, X; Gao, FL; Piao, HB; Cheng, TM; Li, RT
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2003-05-19
DOI: 10.1016/S0960-894X(03)00213-0
卷: 13, 期:10, 页:1729-1732
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]: BIOLOGICAL-ACTIVITIES ; IODIDE DMPP ; BRAIN
英文摘要:

Three series of spirocyclopiperazinium derivatives 5a-d, 6a-f and 17a-d were synthesized and evaluated for their in vivo analgesic activities. Compounds 5a, 17a and 17b exhibited excellent analgesic activity. Two important structure-activity relationships were observed from this study: (1) the quaternary ammonium functionality is a critical pharmacophore for analgesic activity; (2) it is important to adjust the lipophilic property of compounds to improve analgesic activity. (C) 2003 Elsevier Science Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000182913600026
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64221
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Wang, X,Gao, FL,Piao, HB,et al. Unique spirocyclopiperazinium salt. Part 2: Synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2003,13(10):1729-1732.
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