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Unique spirocyclopiperazinium salt III: Further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics
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
2007-11-15
DOI10.1016/j.bmc1.2007.09.026
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
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/400002259/67996
专题北京大学药学院
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
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GB/T 7714
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.
APA Sun, Qi,Yue, Tai-Qin,Ye, Jia,Li, Chang-Ling,Cheng, Tie-Ming,&Li, Run-Tao.(2007).Unique spirocyclopiperazinium salt III: Further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(22),6245-6249.
MLA Sun, Qi,et al."Unique spirocyclopiperazinium salt III: Further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.22(2007):6245-6249.
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