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Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics
Gao, FL; Wang, X; Zhang, HM; Cheng, TM; Li, RT
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2003-05-05
DOI10.1016/S0960-894X(03)00177-X
13期:9页:1535-1537
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 ; IODIDE DMPP ; AFFINITY ; BRAIN
英文摘要

Based on the structure of compound 3, two series of spirocyclopiperazinium derivatives 7a-n and 10a-h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure-activity relationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds 7a-n; the electron-released substitute on the aromatic ring is favorable to increase the analgesic activity. (C) 2003 Elsevier Science Ltd. All rights reserved.

语种英语
WOS记录号WOS:000182418900008
引用统计
被引频次:17[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/400002259/51597
专题北京大学药学院
北京大学药学院_化学生物学系
作者单位Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
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GB/T 7714
Gao, FL,Wang, X,Zhang, HM,et al. Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2003,13(9):1535-1537.
APA Gao, FL,Wang, X,Zhang, HM,Cheng, TM,&Li, RT.(2003).Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,13(9),1535-1537.
MLA Gao, FL,et al."Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 13.9(2003):1535-1537.
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