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Synthesis and Analgesic Activity of Mono-spirocyclopiperazinium Analogues
Liu Wenjun; Wang Xin; Li Gang; Ye Jia; Cheng Tieming; Li Runtao
关键词Mono-spirocyclopiperazinium Analgesic Activity Synthesis Mannich Reaction Structure-activity Relationship
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
2011-12-01
31期:12页:2135-2139
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]BIOLOGICAL-ACTIVITIES ; SALTS ; EPIBATIDINE ; BINDING ; AGONIST ; POTENT
英文摘要

In order to find more potent analgesics, eight new mono-spirocyclopiperazinium analogues were designed and synthesized by selecting compound 1 as lead compound, which was obtained from our previous works. The structures of target compounds were characterized by H-1 NMR, C-13 NMR spectra and elemental analysis or HRMS. The synthesized compounds were evaluated for their in vivo analgesic activity by acetic acid induced writhing test. The results indicate that hydroxyl group on the aryl ring is the key pharmacophore and spirocycloammonium salt framework is favorable for the activity. Enlarging the spiro-ring or introducing substituted group is at a disadvantage.

语种中文
WOS记录号WOS:000299064500022
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52868
专题北京大学药学院
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Liu Wenjun,Wang Xin,Li Gang,et al. Synthesis and Analgesic Activity of Mono-spirocyclopiperazinium Analogues[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2011,31(12):2135-2139.
APA Liu Wenjun,Wang Xin,Li Gang,Ye Jia,Cheng Tieming,&Li Runtao.(2011).Synthesis and Analgesic Activity of Mono-spirocyclopiperazinium Analogues.CHINESE JOURNAL OF ORGANIC CHEMISTRY,31(12),2135-2139.
MLA Liu Wenjun,et al."Synthesis and Analgesic Activity of Mono-spirocyclopiperazinium Analogues".CHINESE JOURNAL OF ORGANIC CHEMISTRY 31.12(2011):2135-2139.
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