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学科主题: 药学
题名:
Unique spirocyclopiperazinium salt III: Further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics
作者: Sun, Qi; Yue, Tai-Qin; Ye, Jia; Li, Chang-Ling; Cheng, Tie-Ming; Li, Run-Tao
关键词: monospirocyclopiperazinium salts ; analgesic ; structure-activity relationship ; synthesis
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2007-11-15
DOI: 10.1016/j.bmc1.2007.09.026
卷: 17, 期:22, 页:6245-6249
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 ; NICOTINIC LIGAND ; IODIDE DMPP ; EPIBATIDINE ; ANALOGS ; BRAIN
英文摘要:

Two novel classes of monospirocyclopiperazinium salts were designed, synthesized, and evaluated for their in vivo analgesic activities. Some interesting structure-activity relationships are revealed: (1) Spirocyclopiperazinium moiety is favorable to improve the analgesic activity; (2) The size and conformation of spirocyclopiperazinium moiety significantly affects the analgesic activity; (3) Phenylethyl group of 3d is a crucial pharmacophore. Among the compounds synthesized, 3d exhibited the most potent activity with low toxicity. Further antinociceptive mechanism studies of 3d showed that these compounds will be a new kind of analgesics. (C) 2007 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000250906200041
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67996
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimetic Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Sun, Qi,Yue, Tai-Qin,Ye, Jia,et al. Unique spirocyclopiperazinium salt III: Further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(22):6245-6249.
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