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Unique spirocyclopiperazinium salt. Part 2: Synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics
Wang, X; Gao, FL; Piao, HB; Cheng, TM; Li, RT
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2003-05-19
DOI10.1016/S0960-894X(03)00213-0
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
引用统计
被引频次:13[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/400002259/64221
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
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.
APA Wang, X,Gao, FL,Piao, HB,Cheng, TM,&Li, RT.(2003).Unique spirocyclopiperazinium salt. Part 2: Synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,13(10),1729-1732.
MLA Wang, X,et al."Unique spirocyclopiperazinium salt. Part 2: Synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 13.10(2003):1729-1732.
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