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Synthesis and structure-activity relationship of di-(3,8-diazabicyclo[3.2.1]octane) diquaternary ammonium salts as unique analgesics
Liu, H; Cheng, TM; Zhang, HM; Li, RT
关键词Analgesic Activities Di-(3 Structure-activity Relationship 8-diazabicyclo[3.2.1]Octane) Diquaternary Ammonium Salts
刊名ARCHIV DER PHARMAZIE
2003-11-01
DOI10.1005/ardp.200300749
336期:11页:510-513
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]BIOLOGICAL-ACTIVITIES ; DERIVATIVES
英文摘要

Based on the structure characteristics of the lead compounds, 1,1′-octanedioyl-4,4′-dimethyl-4,4′-dibenzyl dipiperazinium dibromide (2) and 3,8-disubstituted-3,8-diazabicyclo[3.2.1]octanes (DBO), di-(3,8-diazabicyclo[3.2.1]octane) diquaternary ammonium salts 3a-c were designed and synthesized through a highly practical procedure. Target compounds 3 a-c and the hydrochloride salts of their precursors 10 a-c were evaluated for their in vivo analgesic and sedative activities. Interestingly, the introduction of an endoethylenic bridge in the piperazine of lead compound 2 causes loss of the analgesic activity and increases the toxicity dramatically. This result shows that the flexible conformation of piperazine in compound 2 is favorable for interaction with the receptor, and the quaternization of compounds 10 a-c is the main reason for the toxicity increase.

语种英语
WOS记录号WOS:000187229900003
引用统计
被引频次:4[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/400002259/55424
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
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Liu, H,Cheng, TM,Zhang, HM,et al. Synthesis and structure-activity relationship of di-(3,8-diazabicyclo[3.2.1]octane) diquaternary ammonium salts as unique analgesics[J]. ARCHIV DER PHARMAZIE,2003,336(11):510-513.
APA Liu, H,Cheng, TM,Zhang, HM,&Li, RT.(2003).Synthesis and structure-activity relationship of di-(3,8-diazabicyclo[3.2.1]octane) diquaternary ammonium salts as unique analgesics.ARCHIV DER PHARMAZIE,336(11),510-513.
MLA Liu, H,et al."Synthesis and structure-activity relationship of di-(3,8-diazabicyclo[3.2.1]octane) diquaternary ammonium salts as unique analgesics".ARCHIV DER PHARMAZIE 336.11(2003):510-513.
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